Pub Date : 2022-09-26DOI: 10.2174/2211352520666220926153205
Hesamoddin Hosseinjani, Mahshid Ataei, O. Arasteh, A. Maghsoudi, S. Hassani
The first case of COVID-19 was introduced in China in 2019 and spread rapidly worldwide. Therefore, all researchers worldwide sought ways to treat and prevent the disease. Since production of vaccines and new drugs is time-consuming, a good way is to look at existing drugs to find new effects. Due to the pathogenic mechanism of COVID-19, most of its symptoms, including anosmia, ageusia, and cytokine storm, are dependent on the release of histamine and its activities. Therefore, one category of drugs that may be effective in treating and improving the symptoms of COVID-19 is antihistamines. This paper reviewed studies that have been done so far on the effects of antihistamines, specially famotidine, in COVID-19. A literature search was performed using scientific databases such as PubMed, Web of Science, Scopus, and Google Scholar from beginning up to December 2021. The most relevant articles considering the potential impacts of antihistamines against COVID-19 were collected. In addition to the current medications prescribed for the treatment of SARS-CoV-2, H1 and H2 blockers are promising drugs for repurposing in the COVID-19 remedy. Several studies on famotidine were performed using virtual screening to determine whether they are effective. Many studies have shown that famotidine use improved COVID-19 symptoms and reduced the need for intubation and mortality. However, few studies concluded that famotidine is ineffective. Antihistamines, and specifically famotidine, are effective in reducing COVID-19 symptoms. Therefore, they are a good choice for combination therapy with other drugs to treat COVID-19.
新冠肺炎病例于2019年在中国出现，并在全球迅速传播。因此，全世界的研究人员都在寻找治疗和预防这种疾病的方法。由于疫苗和新药的生产很耗时，一个好方法是研究现有药物以发现新的效果。由于新冠肺炎的致病机制，其大多数症状，包括嗅觉缺失、老年痴呆和细胞因子风暴，都依赖于组胺的释放及其活性。因此，抗组胺药可能对治疗和改善新冠肺炎症状有效。本文回顾了迄今为止关于抗组胺药，特别是法莫替丁对新冠肺炎影响的研究。从2021年初到12月，使用PubMed、Web of Science、Scopus和Google Scholar等科学数据库进行了文献检索。收集了考虑抗组胺药对新冠肺炎的潜在影响的最相关文章。除了目前用于治疗SARS-CoV-2的药物外，H1和H2阻断剂是用于新冠肺炎治疗的有前景的药物。法莫替丁的几项研究是通过虚拟筛选来确定它们是否有效。许多研究表明，法莫替丁的使用改善了新冠肺炎症状，减少了插管需求和死亡率。然而，很少有研究得出法莫替丁无效的结论。抗组胺药，特别是法莫替丁，可有效减少新冠肺炎症状。因此，它们是与其他药物联合治疗新冠肺炎的良好选择。
{"title":"Therapeutic uses of antihistamines in the management of COVID-19: a narrative review","authors":"Hesamoddin Hosseinjani, Mahshid Ataei, O. Arasteh, A. Maghsoudi, S. Hassani","doi":"10.2174/2211352520666220926153205","DOIUrl":"https://doi.org/10.2174/2211352520666220926153205","url":null,"abstract":"\u0000\u0000The first case of COVID-19 was introduced in China in 2019 and spread rapidly worldwide. Therefore, all researchers worldwide sought ways to treat and prevent the disease. Since production of vaccines and new drugs is time-consuming, a good way is to look at existing drugs to find new effects.\u0000\u0000\u0000\u0000Due to the pathogenic mechanism of COVID-19, most of its symptoms, including anosmia, ageusia, and cytokine storm, are dependent on the release of histamine and its activities. Therefore, one category of drugs that may be effective in treating and improving the symptoms of COVID-19 is antihistamines. This paper reviewed studies that have been done so far on the effects of antihistamines, specially famotidine, in COVID-19.\u0000\u0000\u0000\u0000A literature search was performed using scientific databases such as PubMed, Web of Science, Scopus, and Google Scholar from beginning up to December 2021. The most relevant articles considering the potential impacts of antihistamines against COVID-19 were collected.\u0000\u0000\u0000\u0000In addition to the current medications prescribed for the treatment of SARS-CoV-2, H1 and H2 blockers are promising drugs for repurposing in the COVID-19 remedy. Several studies on famotidine were performed using virtual screening to determine whether they are effective. Many studies have shown that famotidine use improved COVID-19 symptoms and reduced the need for intubation and mortality. However, few studies concluded that famotidine is ineffective.\u0000\u0000\u0000\u0000Antihistamines, and specifically famotidine, are effective in reducing COVID-19 symptoms. Therefore, they are a good choice for combination therapy with other drugs to treat COVID-19.\u0000","PeriodicalId":7951,"journal":{"name":"Anti-Infective Agents","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-09-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42604426","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-09-22DOI: 10.2174/2211352520666220922091227
Giorgio Raho, William Cordeddu, D. Firinu, S. Giacco, G. Angioni
Treatment of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection in immuno compromised patients with complete B cell depletion can be really challenging due to the lack of seroconversion and long lasting disease. We describe a case of long-lasting coronavirus disease (COVID-19) in a female patient with rheumatoid arthritis who was treated with rituximab and continued to show B-cell depletion. An ongoing replication of SARS-CoV-2 was demonstrated for a period of 8 months when nasopharyngeal swabs were tested. She was treated once with remdesivir but without lasting resolution, and she was then treated with convalescent plasma but with a similar effect. Only with a combination of both treatments was clinical resolution achieved. The patient's lack of seroconversion and the prolonged course of the disease illustrate the importance of humoral immunity in resolving SARS-CoV-2 infection. This case report highlights challenges in managing immunocompromised hosts, who may act as persistent shedders and sources of transmission. Combination of remdesivir and convalescent plasma resulted successful to achieve clinical resolution of SARS-CoV-2 infection in our patient.
{"title":"Successful combination of remdesivir and convalescent plasma to treat a patient with rituximab-related B-cell deficiency and prolonged COVID-19: A case report","authors":"Giorgio Raho, William Cordeddu, D. Firinu, S. Giacco, G. Angioni","doi":"10.2174/2211352520666220922091227","DOIUrl":"https://doi.org/10.2174/2211352520666220922091227","url":null,"abstract":"\u0000\u0000Treatment of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection in immuno compromised patients with complete B cell depletion can be really challenging due to the lack of seroconversion and long lasting disease.\u0000\u0000\u0000\u0000We describe a case of long-lasting coronavirus disease (COVID-19) in a female patient with rheumatoid arthritis who was treated with rituximab and continued to show B-cell depletion. An ongoing replication of SARS-CoV-2 was demonstrated for a period of 8 months when nasopharyngeal swabs were tested. She was treated once with remdesivir but without lasting resolution, and she was then treated with convalescent plasma but with a similar effect. Only with a combination of both treatments was clinical resolution achieved. The patient's lack of seroconversion and the prolonged course of the disease illustrate the importance of humoral immunity in resolving SARS-CoV-2 infection. This case report highlights challenges in managing immunocompromised hosts, who may act as persistent shedders and sources of transmission.\u0000\u0000\u0000\u0000Combination of remdesivir and convalescent plasma resulted successful to achieve clinical resolution of SARS-CoV-2 infection in our patient.\u0000","PeriodicalId":7951,"journal":{"name":"Anti-Infective Agents","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-09-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44130608","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-08-29DOI: 10.2174/2211352520666220829153943
Faranak Rezaei, Zahra Bakhshiani, S. Fouladi
Since sepsis is a major global health problem, a rapid and correct diagnosis and the initiation of therapy are essential to improve the patient consequences. This study aimed to assess the serum levels of calprotectin and a more widely used sepsis biomarker in the patients with bacterial sepsis (BS). Subjects were classified into BS group with the patients who met the sepsis criteria at the beginning of the study and the control group. We investigated the concentrations of biomarkers in 300 blood samples collected at admission from all patients hospitalized in the Fatemeh Al-Zahra Hospital, Najafabad, Isfahan in April 2019 and April 2020. The microbial etiology in the BS group was confirmed in 35 patients (100%). The most frequently cultivated pathogens were Escherichia coli (n=11). The serum concentrations of calprotectin and CRP were significantly higher in the patients with BS (n= 35) than in the healthy controls (n= 20). Our results suggest that the serum level of calprotectin could have the substantial added value to manage BS which is a reliable biomarker of BS.
由于败血症是一个主要的全球健康问题，快速准确的诊断和治疗对于改善患者的后果至关重要。本研究旨在评估细菌性败血症（BS）患者血清钙卫蛋白和一种更广泛使用的败血症生物标志物的水平。受试者被分为BS组和对照组，其中患者在研究开始时符合败血症标准。我们调查了2019年4月和2020年4月在伊斯法罕纳贾法巴德Fatemeh Al Zahra医院住院的所有患者入院时采集的300份血液样本中的生物标志物浓度。BS组的微生物病因在35名患者中得到证实（100%）。最常培养的病原体是大肠杆菌（n=11）。BS患者（n=35）的血清钙卫蛋白和CRP浓度显著高于健康对照组（n=20）。我们的结果表明，血清钙卫蛋白水平可能对管理BS具有实质性的附加值，这是BS的可靠生物标志物。
{"title":"Calprotectin as a Serodiagnostic Marker for Bacterial Sepsis","authors":"Faranak Rezaei, Zahra Bakhshiani, S. Fouladi","doi":"10.2174/2211352520666220829153943","DOIUrl":"https://doi.org/10.2174/2211352520666220829153943","url":null,"abstract":"\u0000\u0000Since sepsis is a major global health problem, a rapid and correct diagnosis and the initiation of therapy are essential to improve the patient consequences. This study aimed to assess the serum levels of calprotectin and a more widely used sepsis biomarker in the patients with bacterial sepsis (BS).\u0000\u0000\u0000\u0000Subjects were classified into BS group with the patients who met the sepsis criteria at the beginning of the study and the control group. We investigated the concentrations of biomarkers in 300 blood samples collected at admission from all patients hospitalized in the Fatemeh Al-Zahra Hospital, Najafabad, Isfahan in April 2019 and April 2020.\u0000\u0000\u0000\u0000The microbial etiology in the BS group was confirmed in 35 patients (100%). The most frequently cultivated pathogens were Escherichia coli (n=11). The serum concentrations of calprotectin and CRP were significantly higher in the patients with BS (n= 35) than in the healthy controls (n= 20).\u0000\u0000\u0000\u0000Our results suggest that the serum level of calprotectin could have the substantial added value to manage BS which is a reliable biomarker of BS.\u0000","PeriodicalId":7951,"journal":{"name":"Anti-Infective Agents","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-08-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48751355","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-08-22DOI: 10.2174/2211352520666220822145139
R. Kaur, Rajwinder Kaur, Ashlin Varghese, Nidhi Garg, S. Arora
Antibiotics play an essential role in antimicrobial therapy. Among all the medications in children, the most commonly prescribed therapy is antibiotics and is currently the indispensable means to cure transmissible diseases. Several categories of antibiotics have been introduced into clinical practice to treat microbial infections. Reducing the unnecessary use of antibiotics is a global need and priority. This article aims to provide better knowledge and understanding of the impact of the early use of antibiotics. This article highlights the proper use of antibiotics in children, detailing how early and inappropriate use of antibiotics affect the gut microbiome during normal body development and consequently affect the metabolic by way of diabetes mellitus, obesity, and recurrence of infections such as UTI and resistance factors in neonates, infant and developing child, dose requirement, etc. Several new antibiotics in their development stage, newly marketed antibiotics, some recalled and withdrawn from the market are also briefly discussed in this article. This study will help future researchers to explore the latest information about antibiotics used in paediatrics.
{"title":"Antibiotics in Paediatrics: A Boon or a Bane?","authors":"R. Kaur, Rajwinder Kaur, Ashlin Varghese, Nidhi Garg, S. Arora","doi":"10.2174/2211352520666220822145139","DOIUrl":"https://doi.org/10.2174/2211352520666220822145139","url":null,"abstract":"\u0000\u0000Antibiotics play an essential role in antimicrobial therapy. Among all the medications in children, the most commonly prescribed therapy is antibiotics and is currently the indispensable means to cure transmissible diseases. Several categories of antibiotics have been introduced into clinical practice to treat microbial infections. Reducing the unnecessary use of antibiotics is a global need and priority. This article aims to provide better knowledge and understanding of the impact of the early use of antibiotics. This article highlights the proper use of antibiotics in children, detailing how early and inappropriate use of antibiotics affect the gut microbiome during normal body development and consequently affect the metabolic by way of diabetes mellitus, obesity, and recurrence of infections such as UTI and resistance factors in neonates, infant and developing child, dose requirement, etc. Several new antibiotics in their development stage, newly marketed antibiotics, some recalled and withdrawn from the market are also briefly discussed in this article. This study will help future researchers to explore the latest information about antibiotics used in paediatrics.\u0000","PeriodicalId":7951,"journal":{"name":"Anti-Infective Agents","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-08-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48649645","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-08-18DOI: 10.2174/2211352520666220818095716
Mohammad A Al-Kafaween, A. M. Hilmi, H. Al-Jamal
Kelulut and Yemeni Sidr honeys have been documented to have various therapeutic properties. Investigations associated with the medicinal properties and physicochemical characteristics of Kelulut and Yemeni Sidr honey are growing broadly and receiving raised awareness. This study incorporated and analysed the findings on the biological and physicochemical properties of Kelulut and Yemeni Sidr honeys. Kelulut and Yemeni Sidr honeys were found to have a wide variety of biological effects attributed to their physicochemical characteristics. Findings showed that Kelulut and Yemeni Sidr honeys have anti-bacterial, anti-biofilm, anti-virulence, anti-oxidative, anti-cancer, anti-inflammatory, anti-diabetic, anti-obesity and wound-healing properties. The physicochemical properties of Kelulut and Yemeni Sidr honeys were compared and discussed and results revealed that they have high-quality contents and excellent antioxidant sources.
{"title":"PHYSICOCHEMICAL AND THERAPEUTIC PROPERTIES OF MALAYSIAN STINGLESS BEE KELULUT HONEY IN COMPARISON WITH YEMENI SIDR HONEY","authors":"Mohammad A Al-Kafaween, A. M. Hilmi, H. Al-Jamal","doi":"10.2174/2211352520666220818095716","DOIUrl":"https://doi.org/10.2174/2211352520666220818095716","url":null,"abstract":"Kelulut and Yemeni Sidr honeys have been documented to have various therapeutic properties. Investigations associated with the medicinal properties and physicochemical characteristics of Kelulut and Yemeni Sidr honey are growing broadly and receiving raised awareness. This study incorporated and analysed the findings on the biological and physicochemical properties of Kelulut and Yemeni Sidr honeys. Kelulut and Yemeni Sidr honeys were found to have a wide variety of biological effects attributed to their physicochemical characteristics. Findings showed that Kelulut and Yemeni Sidr honeys have anti-bacterial, anti-biofilm, anti-virulence, anti-oxidative, anti-cancer, anti-inflammatory, anti-diabetic, anti-obesity and wound-healing properties. The physicochemical properties of Kelulut and Yemeni Sidr honeys were compared and discussed and results revealed that they have high-quality contents and excellent antioxidant sources.","PeriodicalId":7951,"journal":{"name":"Anti-Infective Agents","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-08-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49560588","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-08-15DOI: 10.2174/2211352520666220815145503
H. Goli, Z. Bazgir, M. Gholami
According to the reports from World Health Organization, increased use of antibiotics and bacterial resistance has become a worldwide issue. Resistance to antimicrobial agents in Escherichia coli clinical strains is increasing. The objective of this study was to determine the antibiotic resistance patterns and frequency of multidrug resistance (MDR) phenotype in Escherichia coli isolated from patients in two major hospitals of Sari, north Iran. In this descriptive-analytical study, a total of 13322 clinical specimens were collected from patients. All the specimens were evaluated to determine the presence of E. coli strains using conventional biochemical tests and API kit. Susceptibility testing against twelve antibiotics was determined using the disk-diffusion method. Results were interpreted in accordance to the Clinical and Laboratory Standard Institute (CLSI) protocol. Out of 13322 studied samples, 964 (7.23%) E. coli strains were identified. In two hospitals, high resistance to ampicillin and cefalexin was presented in 621 (64.4 %) and 402 (41.7 %) isolates, respectively. The highest antibiotic resistance was observed in the burn unit, the burn intensive care unit (ICU) and the burn restoration section, while all the strains (eight) that were isolated from the neonatal-ICU, were sensitive to all the tested antibiotics except cefalexin, nitrofurantoin, nalidixic acid, and ampicillin. Also, strains isolated from urine, wound, stool, and blood samples were resistant to all tested antibiotics. Increased resistance to different antibiotics in burn hospitals has created increasing concern. Very high resistance to some antibiotics indicates that these drugs are misused in therapeutic centers and highlights that infection control measures should be arranged in the ICUs of our hospitals.
{"title":"Two Years Study of Frequency and Antimicrobial Resistance Patterns of Escherichia coli Strains Isolated from Clinical Specimens in Northern Iran","authors":"H. Goli, Z. Bazgir, M. Gholami","doi":"10.2174/2211352520666220815145503","DOIUrl":"https://doi.org/10.2174/2211352520666220815145503","url":null,"abstract":"\u0000\u0000According to the reports from World Health Organization, increased use of antibiotics and bacterial resistance has become a worldwide issue. Resistance to antimicrobial agents in Escherichia coli clinical strains is increasing.\u0000\u0000\u0000\u0000The objective of this study was to determine the antibiotic resistance patterns and frequency of multidrug resistance (MDR) phenotype in Escherichia coli isolated from patients in two major hospitals of Sari, north Iran.\u0000\u0000\u0000\u0000In this descriptive-analytical study, a total of 13322 clinical specimens were collected from patients. All the specimens were evaluated to determine the presence of E. coli strains using conventional biochemical tests and API kit. Susceptibility testing against twelve antibiotics was determined using the disk-diffusion method. Results were interpreted in accordance to the Clinical and Laboratory Standard Institute (CLSI) protocol.\u0000\u0000\u0000\u0000Out of 13322 studied samples, 964 (7.23%) E. coli strains were identified. In two hospitals, high resistance to ampicillin and cefalexin was presented in 621 (64.4 %) and 402 (41.7 %) isolates, respectively. The highest antibiotic resistance was observed in the burn unit, the burn intensive care unit (ICU) and the burn restoration section, while all the strains (eight) that were isolated from the neonatal-ICU, were sensitive to all the tested antibiotics except cefalexin, nitrofurantoin, nalidixic acid, and ampicillin. Also, strains isolated from urine, wound, stool, and blood samples were resistant to all tested antibiotics.\u0000\u0000\u0000\u0000Increased resistance to different antibiotics in burn hospitals has created increasing concern. Very high resistance to some antibiotics indicates that these drugs are misused in therapeutic centers and highlights that infection control measures should be arranged in the ICUs of our hospitals.\u0000","PeriodicalId":7951,"journal":{"name":"Anti-Infective Agents","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-08-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43248004","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Coronavirus disease 2019 (COVID-19) is caused by the severe acute respiratory syndrome coronavirus-2 (SARS, CoV-2), and patients with COVID-19 are managed mainly using repurposed conventional drugs, which target the viral entry and viral replication of SARS CoV-2 along with standard care and supportive therapy. This review article focuses on the potential benefits of black seeds (Nigella sativa) observed in clinical and in silico molecular docking studies of COVID-19. The literature was searched using databases such as LitCOVID, Web of Science, Google Scholar, bioRxiv, medRxiv, Science Direct, EBSCO, Scopus, EMBASE, and reference lists to identify published manuscripts or preprints related to the prevention or treatment of COVID-19 with black seeds (N. sativa) or their phytoconstituents. Various clinical studies and in silico molecular docking studies determined that black seeds (N. sativa) and their bioactive phytoconstituents have potential activity against SARS CoV-2 infection. Patients with COVID-19 could be managed using black seeds (N. sativa) along with supportive care, which would speed up the recovery and decrease the mortality rate. More randomized controlled clinical trials would further establish the safety and efficacy of N. sativa in COVID-19 patients.
{"title":"Therapeutic Potentials of Black Seeds (Nigella sativa) in the Management of COVID-19 -A Review of Clinical and In-silico Studies","authors":"Naina Mohamed Pakkir Maideen, Rajkapoor Balasubramaniam, Sudha Muthusamy, Mirunalini Gobinath, Mohamed Rafiullah","doi":"10.2174/2211352520666220802150156","DOIUrl":"https://doi.org/10.2174/2211352520666220802150156","url":null,"abstract":"\u0000\u0000Coronavirus disease 2019 (COVID-19) is caused by the severe acute respiratory syndrome coronavirus-2 (SARS, CoV-2), and patients with COVID-19 are managed mainly using repurposed conventional drugs, which target the viral entry and viral replication of SARS CoV-2 along with standard care and supportive therapy.\u0000\u0000\u0000\u0000This review article focuses on the potential benefits of black seeds (Nigella sativa) observed in clinical and in silico molecular docking studies of COVID-19.\u0000\u0000\u0000\u0000The literature was searched using databases such as LitCOVID, Web of Science, Google Scholar, bioRxiv, medRxiv, Science Direct, EBSCO, Scopus, EMBASE, and reference lists to identify published manuscripts or preprints related to the prevention or treatment of COVID-19 with black seeds (N. sativa) or their phytoconstituents.\u0000\u0000\u0000\u0000Various clinical studies and in silico molecular docking studies determined that black seeds (N. sativa) and their bioactive phytoconstituents have potential activity against SARS CoV-2 infection.\u0000\u0000\u0000\u0000Patients with COVID-19 could be managed using black seeds (N. sativa) along with supportive care, which would speed up the recovery and decrease the mortality rate. More randomized controlled clinical trials would further establish the safety and efficacy of N. sativa in COVID-19 patients.\u0000","PeriodicalId":7951,"journal":{"name":"Anti-Infective Agents","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-08-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42314039","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Methicillin-resistant Staphylococcus aureus (MRSA) is a gram-positive strain whose resistance against existing antibiotics is a major concern for the researchers across the globe. Gram-positive infections, particularly methicillin-resistant Staphylococcus aureus spreading among S. aureus isolates, observed to increase exponentially from 29% in 2009 to 47% in 2014. Literature reviews revealed about 13-74% of worldwide S. aureus strains are Methicillin-resistant. In this article, we have summarized the mechanism of bacterium resistance, molecular targets to treat MRSA, and the activity of reported pyridine and pyrimidine derivatives against methicillin-resistant Staphylococcus aureus. The data collected for this study from online peer reviewed research articles and Molecular-docking study of reported anti-MRSA agents performed by using Maestro Module of Schrodinger software. Results of in silico studies showed that some pyridine derivatives having better binding interactions than standard anti-MRSA agents. Molecular docking studies of reported pyridine derivatives resulted in excellent hits for the development of novel anti- MRSA agents. Overall, this study will be immense importance for researchers working in design and development of target based anti-MRSA agents.
{"title":"A review of pyridine and pyrimidine derivatives as anti-MRSA agents","authors":"Adarsh Kumar, Ankit Kumar Singh, Suresh Thareja, Pradeep Kumar","doi":"10.2174/2211352520666220705085733","DOIUrl":"https://doi.org/10.2174/2211352520666220705085733","url":null,"abstract":"\u0000\u0000Methicillin-resistant Staphylococcus aureus (MRSA) is a gram-positive strain whose resistance against existing antibiotics is a major concern for the researchers across the globe. Gram-positive infections, particularly methicillin-resistant Staphylococcus aureus spreading among S. aureus isolates, observed to increase exponentially from 29% in 2009 to 47% in 2014. Literature reviews revealed about 13-74% of worldwide S. aureus strains are Methicillin-resistant.\u0000\u0000\u0000\u0000In this article, we have summarized the mechanism of bacterium resistance, molecular targets to treat MRSA, and the activity of reported pyridine and pyrimidine derivatives against methicillin-resistant Staphylococcus aureus.\u0000\u0000\u0000\u0000The data collected for this study from online peer reviewed research articles and Molecular-docking study of reported anti-MRSA agents performed by using Maestro Module of Schrodinger software. Results of in silico studies showed that some pyridine derivatives having better binding interactions than standard anti-MRSA agents.\u0000\u0000\u0000\u0000Molecular docking studies of reported pyridine derivatives resulted in excellent hits for the development of novel anti- MRSA agents. Overall, this study will be immense importance for researchers working in design and development of target based anti-MRSA agents.\u0000","PeriodicalId":7951,"journal":{"name":"Anti-Infective Agents","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-07-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43932991","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-06-27DOI: 10.2174/2211352520666220627153144
N. R. Babu, R. Raju, R. R. Alavala, G. K. Rao, P. K. Desu, J. Namratha, V. Muralidharan
Tuberculosis is a highly contagious disease that is one of the major causes of mortality worldwide and the leading infectious organism-related cause of death. Various tetrazole and quinazoline compounds have been successfully developed in the past for tuberculosis treatment. In this case, we planned to design the hybrid moieties by combining both tetrazole and quinazoline nucleus to create novel compounds with increased activity. 6, 6-dimethyl-5, 6, 7, 9–tetrahydrotetrazolo [5, 1-b] Quinazolin-8(4H) -one derivatives were synthesized, characterized by using spectral data. The antitubercular activity of the synthesised compounds was tested against the H37RV strain of Mycobacterium tuberculosis. In order to identify the interactions with the target protein Mtb Pks13 Thioesterase domain in complex with inhibitor, docking analysis of the final compounds was performed (Protein data bank ID: 5V41). To verify their drug-like potential, the synthesised compounds were subjected to Pharmacokinetic prediction experiments. Zebrafish larvae had been used to test the teratogenicity of the synthesised compounds. At 6.25 µg/mL, compounds F4 and F7 exhibited good efficacy against Mycobacterium tuberculosis strains. Docking studies aided in determining the most likely binding mode within the binding cavity of the concerned target protein. Compounds containing p-fluorophenyl and p-nitrophenyl groups as substituents were found to have excellent anti-tubercular activity.
{"title":"Synthesis, Characterization and Antitubercular Evaluation of Tetrahydrotetrazolo Quinazoline Derivatives","authors":"N. R. Babu, R. Raju, R. R. Alavala, G. K. Rao, P. K. Desu, J. Namratha, V. Muralidharan","doi":"10.2174/2211352520666220627153144","DOIUrl":"https://doi.org/10.2174/2211352520666220627153144","url":null,"abstract":"\u0000\u0000Tuberculosis is a highly contagious disease that is one of the major causes of mortality worldwide and the leading infectious organism-related cause of death. Various tetrazole and quinazoline compounds have been successfully developed in the past for tuberculosis treatment. In this case, we planned to design the hybrid moieties by combining both tetrazole and quinazoline nucleus to create novel compounds with increased activity.\u0000\u0000\u0000\u00006, 6-dimethyl-5, 6, 7, 9–tetrahydrotetrazolo [5, 1-b] Quinazolin-8(4H) -one derivatives were synthesized, characterized by using spectral data. The antitubercular activity of the synthesised compounds was tested against the H37RV strain of Mycobacterium tuberculosis. In order to identify the interactions with the target protein Mtb Pks13 Thioesterase domain in complex with inhibitor, docking analysis of the final compounds was performed (Protein data bank ID: 5V41). To verify their drug-like potential, the synthesised compounds were subjected to Pharmacokinetic prediction experiments. Zebrafish larvae had been used to test the teratogenicity of the synthesised compounds.\u0000\u0000\u0000\u0000At 6.25 µg/mL, compounds F4 and F7 exhibited good efficacy against Mycobacterium tuberculosis strains. Docking studies aided in determining the most likely binding mode within the binding cavity of the concerned target protein.\u0000\u0000\u0000\u0000Compounds containing p-fluorophenyl and p-nitrophenyl groups as substituents were found to have excellent anti-tubercular activity.\u0000","PeriodicalId":7951,"journal":{"name":"Anti-Infective Agents","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-06-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45716946","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-06-16DOI: 10.2174/2211352520666220616105540
N. Desai, A. Khasiya, B. Dave, V. Khedkar
In the past few decades, mankind is suffering from tormented life-threatening infectious diseases caused by multidrug-resistant bacteria. As a result, new antimicrobial classes with distinct modes of action are required to combat multidrug-resistant infections. The pyrazole-based pyrimidine and pyrazolone motifs were synthesized, characterized, and screened for their antimicrobial activity. Molecular docking was carried out for the development of antimicrobial agents based on the results of biological activity obtained. : We have synthesized a new series of pyrazole containing pyrimidine-pyrazolone hybrids by using multi-step reactions in the search of antimicrobial agents (7a-o). The structures were determined by 1H NMR, 13C NMR, IR, and mass spectroscopy techniques. Moreover, synthesized compounds were evaluated for their antimicrobial activity by using serial Broth dilution method. Antimicrobial activity of synthesized compounds has been tested against bacterial and fungal strains. Compound 7o was most effective against S. aureus with MIC = 0.096 M/mL. A molecular docking study against microbial DNA gyrase revealed important information about the mechanisms underlying antimicrobial efficacy. Through significant interactions with active site residues, all of the compounds were able to dock well into the enzyme's active site. Furthermore, Compounds 7a (0.531 M/mL), 7b (0.456 M/mL), and 7m (0.485 M/mL) showed excellent antifungal activity against C. albicans compared to the positive control griseofulvin. It has been concluded that compounds containing electron-donating groups are found to be most active against bacterial strains while compounds having both electron-donating as well as electron-withdrawing groups are most favorable for antifungal activity.
{"title":"Synthesis, characterization in vitro antimicrobial evaluation and in silico approach of molecular docking of pyrazole based pyrimidine and pyrazolone motifs","authors":"N. Desai, A. Khasiya, B. Dave, V. Khedkar","doi":"10.2174/2211352520666220616105540","DOIUrl":"https://doi.org/10.2174/2211352520666220616105540","url":null,"abstract":"\u0000\u0000In the past few decades, mankind is suffering from tormented life-threatening infectious diseases caused by multidrug-resistant bacteria. As a result, new antimicrobial classes with distinct modes of action are required to combat multidrug-resistant infections.\u0000\u0000\u0000\u0000The pyrazole-based pyrimidine and pyrazolone motifs were synthesized, characterized, and screened for their antimicrobial activity. Molecular docking was carried out for the development of antimicrobial agents based on the results of biological activity obtained.\u0000\u0000\u0000\u0000: We have synthesized a new series of pyrazole containing pyrimidine-pyrazolone hybrids by using multi-step reactions in the search of antimicrobial agents (7a-o). The structures were determined by 1H NMR, 13C NMR, IR, and mass spectroscopy techniques. Moreover, synthesized compounds were evaluated for their antimicrobial activity by using serial Broth dilution method.\u0000\u0000\u0000\u0000Antimicrobial activity of synthesized compounds has been tested against bacterial and fungal strains. Compound 7o was most effective against S. aureus with MIC = 0.096 M/mL. A molecular docking study against microbial DNA gyrase revealed important information about the mechanisms underlying antimicrobial efficacy. Through significant interactions with active site residues, all of the compounds were able to dock well into the enzyme's active site. Furthermore, Compounds 7a (0.531 M/mL), 7b (0.456 M/mL), and 7m (0.485 M/mL) showed excellent antifungal activity against C. albicans compared to the positive control griseofulvin.\u0000\u0000\u0000\u0000It has been concluded that compounds containing electron-donating groups are found to be most active against bacterial strains while compounds having both electron-donating as well as electron-withdrawing groups are most favorable for antifungal activity.\u0000","PeriodicalId":7951,"journal":{"name":"Anti-Infective Agents","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-06-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45883465","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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