Pub Date : 2022-01-01DOI: 10.14233/ajomc.2022.7-1-sp4.pp93-96
{"title":"Use of Crumb Rubber as Replacement Over Aggregate in Concrete","authors":"","doi":"10.14233/ajomc.2022.7-1-sp4.pp93-96","DOIUrl":"https://doi.org/10.14233/ajomc.2022.7-1-sp4.pp93-96","url":null,"abstract":"","PeriodicalId":8544,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"456 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83063787","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 : 2022-01-01DOI: 10.14233/ajomc.2022.ajomc-p373
V. Saini, A. Goyal, Ajay Kumar
Isoniazid (INH) is one of the most successful tuberculosis medications in the market today. In particular, isoniazid is used as a prophylaxis medication to avoid resurgence of illness in those who have underlying Mycobacterium tuberculosis (MTB) infection. The mode of action of isoniazid is complicated and incorporates a number of distinct aspects in which various biomolecular routes are impacted, including mycolic acid production. Catalase-peroxidase (KatG) activates the prodrug isoniazid and enzymes such as β-ketoacyl ACP synthase (KasA) and enoyl acyl carrier protein (ACP) reductase target the active isoniazid products. Various genes in diverse biochemical networks and pathways are involved in the physiological mechanisms of isoniazid resistance. Isoniazid resistance is the most common of all clinical drug-resistant isolates, with incidence in some areas of up to 20 to 30%. In this review article, several existing components that may influence to the complexities of isoniazid function including mechanism of action, resistance mechanisms in MTB, along with their history, different synthetic procedures, uses, dosage forms, side effects, adverse drug reactions, physico-chemical characteristics, ADME properties, contraindications as well as future perspectives are discussed. Studies of pharmacokinetics have found that the cause of the drug mediated hepatotoxicity is possible by metabolism of isoniazid. Because of inter-individual heterogeneity of polymorphism that affect isoniazid metabolism rates, customized medicines may be required in various populations to prevent hepatotoxicity. The isoniazid multidrug combination treatment which would proved to be effective tuberculosis treatment in future. Further exploration is needed for better comprehension of pathogenesis mechanism of Mycobacterium tuberculosis (MTB) and drug resistance studies are required for building up better therapeutics and diagnostic against tuberculosis.
{"title":"Isoniazid: An Exploratory Review","authors":"V. Saini, A. Goyal, Ajay Kumar","doi":"10.14233/ajomc.2022.ajomc-p373","DOIUrl":"https://doi.org/10.14233/ajomc.2022.ajomc-p373","url":null,"abstract":"Isoniazid (INH) is one of the most successful tuberculosis medications in the market today. In particular, isoniazid is used as a prophylaxis medication to avoid resurgence of illness in those who have underlying Mycobacterium tuberculosis (MTB) infection. The mode of action of isoniazid is complicated and incorporates a number of distinct aspects in which various biomolecular routes are impacted, including mycolic acid production. Catalase-peroxidase (KatG) activates the prodrug isoniazid and enzymes such as β-ketoacyl ACP synthase (KasA) and enoyl acyl carrier protein (ACP) reductase target the active isoniazid products. Various genes in diverse biochemical networks and pathways are involved in the physiological mechanisms of isoniazid resistance. Isoniazid resistance is the most common of all clinical drug-resistant isolates, with incidence in some areas of up to 20 to 30%. In this review article, several existing components that may influence to the complexities of isoniazid function including mechanism of action, resistance mechanisms in MTB, along with their history, different synthetic procedures, uses, dosage forms, side effects, adverse drug reactions, physico-chemical characteristics, ADME properties, contraindications as well as future perspectives are discussed. Studies of pharmacokinetics have found that the cause of the drug mediated hepatotoxicity is possible by metabolism of isoniazid. Because of inter-individual heterogeneity of polymorphism that affect isoniazid metabolism rates, customized medicines may be required in various populations to prevent hepatotoxicity. The isoniazid multidrug combination treatment which would proved to be effective tuberculosis treatment in future. Further exploration is needed for better comprehension of pathogenesis mechanism of Mycobacterium tuberculosis (MTB) and drug resistance studies are required for building up better therapeutics and diagnostic against tuberculosis.","PeriodicalId":8544,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83331553","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 : 2022-01-01DOI: 10.14233/ajomc.2022.7-1-sp4.pp227-229
{"title":"Comparison of Hardnessforal-7075 Thixoformed upto Recrystallization Temperatures","authors":"","doi":"10.14233/ajomc.2022.7-1-sp4.pp227-229","DOIUrl":"https://doi.org/10.14233/ajomc.2022.7-1-sp4.pp227-229","url":null,"abstract":"","PeriodicalId":8544,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"45 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83823731","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 : 2022-01-01DOI: 10.14233/ajomc.2022.7-1-sp4.pp76-78
{"title":"Review Paper on Advanced Technologies Used in Retrofitting","authors":"","doi":"10.14233/ajomc.2022.7-1-sp4.pp76-78","DOIUrl":"https://doi.org/10.14233/ajomc.2022.7-1-sp4.pp76-78","url":null,"abstract":"","PeriodicalId":8544,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"33 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78348297","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 : 2022-01-01DOI: 10.14233/ajomc.2022.7-1-sp4.pp205-209
{"title":"A Review Paper on Abrasive Water Jet Machining","authors":"","doi":"10.14233/ajomc.2022.7-1-sp4.pp205-209","DOIUrl":"https://doi.org/10.14233/ajomc.2022.7-1-sp4.pp205-209","url":null,"abstract":"","PeriodicalId":8544,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"224 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74464417","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 : 2022-01-01DOI: 10.14233/ajomc.2022.7-1-sp4.pp79-82
{"title":"A Review on Seismic Evaluation of RC Building","authors":"","doi":"10.14233/ajomc.2022.7-1-sp4.pp79-82","DOIUrl":"https://doi.org/10.14233/ajomc.2022.7-1-sp4.pp79-82","url":null,"abstract":"","PeriodicalId":8544,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"14 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75417242","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 : 2022-01-01DOI: 10.14233/ajomc.2022.ajomc-p363
Nitin J. Deshmukh, L. Soni
The aim of this work was to evaluate the physico-chemical, pharmacokinetic parameters (absorption, distribution, metabolism, excretion and toxicity) and pharmacodynamic parameters (bioactivity and adverse reactions) of substituted thiadiazole by means of in silico computational prediction. Online softwares such as Pre-ADMET, Molinspiration and rule of five were used for the analysis. Substituted thiadiazole fits the characteristics of drug-likeness, pharmacokinetic properties appropriate to the predicted patterns and activities within the scope for the treatment of infection in the stomach or duodenum (first part of the small intestine), gastritis and trypanosomiasis. Therefore, in silico results allow us to conclude that substituted thiadiazole is predicted to be a potential future drug candidate, due to its relevant Drug-likeness profile, bioavailability, excellent liposolubility and adequate pharmacokinetics, including at the level of CNS, penetrating the blood-brain barrier. Molecular docking studies have also been performed to screen the antibacterial and antifungal activities of the 50 designed compounds against protein targets Helicobacter pylori α-carbonic anhydrase (PDB: 5TUO) and Trypanosoma brucei Pteridine Reductase (PTR1) (PDB: 4WCD) respectively. Among all the compounds C11 exhibited the most significant affinity score against Helicobacter pylori α-carbonic anhydrase and C37 exhibited the most significant affinity score against Trypanosoma brucei pteridine reductase (PTR1) best significant hydrogen bonds interaction at the active site of protein.
本研究的目的是利用计算机计算预测方法评价取代噻二唑的理化、药代动力学参数(吸收、分布、代谢、排泄和毒性)和药效学参数(生物活性和不良反应)。使用Pre-ADMET、Molinspiration、rule of five等在线软件进行分析。替代噻二唑在治疗胃或十二指肠(小肠的第一部分)感染、胃炎和锥虫病的范围内，具有药物相似、药代动力学性质与预测模式和活性相适应的特点。因此，硅实验结果使我们得出结论，由于其相关的药物相似性、生物利用度、优异的脂溶性和充分的药代动力学，包括在中枢神经系统水平，穿透血脑屏障，取代噻二唑被预测为潜在的未来候选药物。通过分子对接研究，筛选了50种化合物对蛋白质靶点幽门螺杆菌α-碳酸酐酶(PDB: 5TUO)和布鲁氏锥虫Pteridine Reductase (PDB: 4WCD)的抑菌和抗真菌活性。其中C11对幽门螺杆菌α-碳酸酐酶亲和性最强，C37对布鲁氏锥虫翼基化酶(PTR1)亲和性最强，蛋白活性位点氢键相互作用最显著。
{"title":"Prediction of in silico ADMET Properties and Molecular Docking Study of Substituted\u0000Thiadiazole for Screening of Antibacterial and Antifungal Activities against Protein Targets\u0000Helicobacter pylori α-Carbonic Anhydrase and Trypanosoma brucei Pteridine Reductase","authors":"Nitin J. Deshmukh, L. Soni","doi":"10.14233/ajomc.2022.ajomc-p363","DOIUrl":"https://doi.org/10.14233/ajomc.2022.ajomc-p363","url":null,"abstract":"The aim of this work was to evaluate the physico-chemical, pharmacokinetic parameters (absorption, distribution, metabolism, excretion and toxicity) and pharmacodynamic parameters (bioactivity and adverse reactions) of substituted thiadiazole by means of in silico computational prediction. Online softwares such as Pre-ADMET, Molinspiration and rule of five were used for the analysis. Substituted thiadiazole fits the characteristics of drug-likeness, pharmacokinetic properties appropriate to the predicted patterns and activities within the scope for the treatment of infection in the stomach or duodenum (first part of the small intestine), gastritis and trypanosomiasis. Therefore, in silico results allow us to conclude that substituted thiadiazole is predicted to be a potential future drug candidate, due to its relevant Drug-likeness profile, bioavailability, excellent liposolubility and adequate pharmacokinetics, including at the level of CNS, penetrating the blood-brain barrier. Molecular docking studies have also been performed to screen the antibacterial and antifungal activities of the 50 designed compounds against protein targets Helicobacter pylori α-carbonic anhydrase (PDB: 5TUO) and Trypanosoma brucei Pteridine Reductase (PTR1) (PDB: 4WCD) respectively. Among all the compounds C11 exhibited the most significant affinity score against Helicobacter pylori α-carbonic anhydrase and C37 exhibited the most significant affinity score against Trypanosoma brucei pteridine reductase (PTR1) best significant hydrogen bonds interaction at the active site of protein.","PeriodicalId":8544,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"13 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75870779","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 : 2022-01-01DOI: 10.14233/ajomc.2022.7-1-sp4.pp20-23
{"title":"A Review on the Behaviour of Tubular Section and Conventional Section","authors":"","doi":"10.14233/ajomc.2022.7-1-sp4.pp20-23","DOIUrl":"https://doi.org/10.14233/ajomc.2022.7-1-sp4.pp20-23","url":null,"abstract":"","PeriodicalId":8544,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"134 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75035282","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 : 2022-01-01DOI: 10.14233/ajomc.2022.7-1-sp4.pp1-4
{"title":"Plastic Bottles Applicability for Local Construction: A Survey","authors":"","doi":"10.14233/ajomc.2022.7-1-sp4.pp1-4","DOIUrl":"https://doi.org/10.14233/ajomc.2022.7-1-sp4.pp1-4","url":null,"abstract":"","PeriodicalId":8544,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"543 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78168094","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 : 2022-01-01DOI: 10.14233/ajomc.2022.7-1-sp4.pp248-250
{"title":"Understanding the Make-or-buy Decision Strategy: A Brief Communication","authors":"","doi":"10.14233/ajomc.2022.7-1-sp4.pp248-250","DOIUrl":"https://doi.org/10.14233/ajomc.2022.7-1-sp4.pp248-250","url":null,"abstract":"","PeriodicalId":8544,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"114 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86994268","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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