Organic and Medicinal chemistry international Journal is an open access journal that is committed to publish the papers on various topics of chemistry, especially synthetic organic chemistry, and pharmacology and various other biological specialties
{"title":"Synthesis, Characterization, Aggregation Behavior, Antifungal and Antibacterial Studies of a Novel Tetra-Metronidazole Substituted Zinc (II) Phthalocyanine","authors":"Asma Ibrahmi, Safa Belaiba, Manel Ben Mansour, Mohamed Adnen Hadj Ayed, Jameleddine Khiari","doi":"10.19080/omcij.2023.12.555841","DOIUrl":"https://doi.org/10.19080/omcij.2023.12.555841","url":null,"abstract":"Organic and Medicinal chemistry international Journal is an open access journal that is committed to publish the papers on various topics of chemistry, especially synthetic organic chemistry, and pharmacology and various other biological specialties","PeriodicalId":19547,"journal":{"name":"Organic & Medicinal Chemistry International Journal","volume":"9 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-08-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135165721","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 : 2020-12-01DOI: 10.19080/omcij.2020.10.555783
N. Riaz
A series of new N-substituted-(4-bromophenyl)-4-ethoxybenzenesulfonamides (5a-o) were synthesized and evaluated for enzyme inhibition potential. The task was accomplished by the reaction of 4-bromobenzenesulfonyl chloride a. with 4-ethoxyaniline b. to get the intermediate 4-bromophenyl-4-ethoxybenzenesulfonamide in the first step. The compound 3 on further reaction with different electrophiles (4a-o) yielded the target compounds 5a-o, which were characterized with the help of FTIR, 1 H-, 13 C-NMR spectroscopic and EI-MS & HR-EI-MS spectrometric data. These sulfonamides (5a-o) were evaluated for their acetylcholinesterase (AChE) and α -glucosidase inhibitory potential. Compounds 5l, 5n, 5g, 5j and 5h exhibited excellent potential against AChE with IC 50 values of 52.63 ± 0.14, 82.75 ± 0.16, 92.13 ± 0.15, 92.52 ± 0.16 and 98.72 ± 0.12 µM, respectively. Compounds 5h, 5j, 5c, 5d and 5l were found potent inhibitors of α -glucosidase with IC 50 values of 57.38 ± 0.19, 123.36 ± 0.19, 123.42 ± 0.19, 124.35 ± 0.15 and 124.74 ± 0.18 µM, respectively. The activity results were also substantiated by in silico studies.
{"title":"Enzyme Inhibition and In Silico Studies of New Synthetic N-Substituted- (4-Bromophenyl)-4-Ethoxybenzenesulfonamides","authors":"N. Riaz","doi":"10.19080/omcij.2020.10.555783","DOIUrl":"https://doi.org/10.19080/omcij.2020.10.555783","url":null,"abstract":"A series of new N-substituted-(4-bromophenyl)-4-ethoxybenzenesulfonamides (5a-o) were synthesized and evaluated for enzyme inhibition potential. The task was accomplished by the reaction of 4-bromobenzenesulfonyl chloride a. with 4-ethoxyaniline b. to get the intermediate 4-bromophenyl-4-ethoxybenzenesulfonamide in the first step. The compound 3 on further reaction with different electrophiles (4a-o) yielded the target compounds 5a-o, which were characterized with the help of FTIR, 1 H-, 13 C-NMR spectroscopic and EI-MS & HR-EI-MS spectrometric data. These sulfonamides (5a-o) were evaluated for their acetylcholinesterase (AChE) and α -glucosidase inhibitory potential. Compounds 5l, 5n, 5g, 5j and 5h exhibited excellent potential against AChE with IC 50 values of 52.63 ± 0.14, 82.75 ± 0.16, 92.13 ± 0.15, 92.52 ± 0.16 and 98.72 ± 0.12 µM, respectively. Compounds 5h, 5j, 5c, 5d and 5l were found potent inhibitors of α -glucosidase with IC 50 values of 57.38 ± 0.19, 123.36 ± 0.19, 123.42 ± 0.19, 124.35 ± 0.15 and 124.74 ± 0.18 µM, respectively. The activity results were also substantiated by in silico studies.","PeriodicalId":19547,"journal":{"name":"Organic & Medicinal Chemistry International Journal","volume":"40 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74195835","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 : 2020-12-01DOI: 10.19080/omcij.2020.10.555784
Sandile B Simelane
Tuberculosis (TB) is one of the world’s most deadly infectious diseases, causing 1.2 million deaths in 2018. TB is the leading cause of death from a single infectious agent, ahead of HIV/AIDS. The African continent bears the highest global TB/HIV burden and over 50% of TB cases in sub-Saharan Africa are co-infected with HIV. With an estimated 1.7 billion people (23% of the world’s population) with latent TB infection, there is an urgent need to develop drugs that will eradicate or control the disease. Moreover, the emergence of multi-drug resistant tuberculosis (MDR-TB) and extensively drug resistant tuberculosis (XDR-TB) have accelerated the need for new antitubercular agents with novel biological targets and different mechanism of action. Among the wide spectra of heterocyclic compounds, benzopyran derivatives have displayed diverse biological applications. Found in many natural products, this scaffold together with its synthetic analogs has intrigued medicinal chemists to explore its applicability as anti-TB drugs. To further intensify research in this area, there is need to gather the latest information on benzopyrans as antimycobacterial agents. This review presents an overview of recent developments (2000 -2018) in anti-TB applications of benzopyrans, both the synthetic analogs and isolated natural products. The objective of this review is to focus on active benzopyran analogs and structure activity relationship (SAR) analysis. We envisage that this review will be helpful in rational design of potent, less toxic benzopyran-based anti-TB drug candidates. a the of mycobacterial cell wall lipid biosynthesis. oxo-4H-chromene-3-carbonitriles with ethyl cyanoacetate. The compounds were investigated for their antitubercular activity against H 37 Rv at a concentration of 62.5μ g/mL, using the L-J method. In this experiment, compound 29 was the most effective against H 37 Rv strain with 99% inhibition [70].
{"title":"Benzopyran-Core as an Antimycobacterial Agent","authors":"Sandile B Simelane","doi":"10.19080/omcij.2020.10.555784","DOIUrl":"https://doi.org/10.19080/omcij.2020.10.555784","url":null,"abstract":"Tuberculosis (TB) is one of the world’s most deadly infectious diseases, causing 1.2 million deaths in 2018. TB is the leading cause of death from a single infectious agent, ahead of HIV/AIDS. The African continent bears the highest global TB/HIV burden and over 50% of TB cases in sub-Saharan Africa are co-infected with HIV. With an estimated 1.7 billion people (23% of the world’s population) with latent TB infection, there is an urgent need to develop drugs that will eradicate or control the disease. Moreover, the emergence of multi-drug resistant tuberculosis (MDR-TB) and extensively drug resistant tuberculosis (XDR-TB) have accelerated the need for new antitubercular agents with novel biological targets and different mechanism of action. Among the wide spectra of heterocyclic compounds, benzopyran derivatives have displayed diverse biological applications. Found in many natural products, this scaffold together with its synthetic analogs has intrigued medicinal chemists to explore its applicability as anti-TB drugs. To further intensify research in this area, there is need to gather the latest information on benzopyrans as antimycobacterial agents. This review presents an overview of recent developments (2000 -2018) in anti-TB applications of benzopyrans, both the synthetic analogs and isolated natural products. The objective of this review is to focus on active benzopyran analogs and structure activity relationship (SAR) analysis. We envisage that this review will be helpful in rational design of potent, less toxic benzopyran-based anti-TB drug candidates. a the of mycobacterial cell wall lipid biosynthesis. oxo-4H-chromene-3-carbonitriles with ethyl cyanoacetate. The compounds were investigated for their antitubercular activity against H 37 Rv at a concentration of 62.5μ g/mL, using the L-J method. In this experiment, compound 29 was the most effective against H 37 Rv strain with 99% inhibition [70].","PeriodicalId":19547,"journal":{"name":"Organic & Medicinal Chemistry International Journal","volume":"22 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73036102","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 : 2020-11-25DOI: 10.19080/omcij.2020.10.555782
Daniela Vieira
Biomaterials to regenerate bone have been gaining great visibility in tissue engineering. The design of a material like bone is a great challenge, especially when combining the ideal mechanical strength, porosity, and bioactivity. This work focused on the development of a new candidate for bone substitute combining hydroxyapatite (HAp) and silk fibroin (SF). The silk fibroin, obtained from the cocoons of the silkworm (Bombyx mori), was dissolved using a ternary solution of calcium, ethanol, and water. HAp was co-precipitated dropping phosphate solution (Na2HPO4) in SF at a constant stirring. The final composite, 75%HAp/25%SF, were framed using a hydraulic system varying the pressure to find the best candidate. Physical and chemical characterizations were evaluated, as well as the bioactivity and cytotoxicity. Results showed excellent chemical and physical properties, like the trabecular bone. The 75%HAp/25%SF biocomposite was safe to CHO cells and presented great bioactivity being an alternative candidate to the bone regeneration field.
{"title":"A New Approach to Design Hydroxyapatite and Silk Fibroin Bone Substitutes","authors":"Daniela Vieira","doi":"10.19080/omcij.2020.10.555782","DOIUrl":"https://doi.org/10.19080/omcij.2020.10.555782","url":null,"abstract":"Biomaterials to regenerate bone have been gaining great visibility in tissue engineering. The design of a material like bone is a great challenge, especially when combining the ideal mechanical strength, porosity, and bioactivity. This work focused on the development of a new candidate for bone substitute combining hydroxyapatite (HAp) and silk fibroin (SF). The silk fibroin, obtained from the cocoons of the silkworm (Bombyx mori), was dissolved using a ternary solution of calcium, ethanol, and water. HAp was co-precipitated dropping phosphate solution (Na2HPO4) in SF at a constant stirring. The final composite, 75%HAp/25%SF, were framed using a hydraulic system varying the pressure to find the best candidate. Physical and chemical characterizations were evaluated, as well as the bioactivity and cytotoxicity. Results showed excellent chemical and physical properties, like the trabecular bone. The 75%HAp/25%SF biocomposite was safe to CHO cells and presented great bioactivity being an alternative candidate to the bone regeneration field.","PeriodicalId":19547,"journal":{"name":"Organic & Medicinal Chemistry International Journal","volume":"54 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-11-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85818136","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 : 2020-11-16DOI: 10.19080/omcij.2020.10.555781
Derenik S Khachatryan
Here we report on a strategy based on the capabilities of 2D NMR spectroscopy, which focuses on determining the exact structures of promising HDAC / VEGF-2 inhibitors and intermediate N- or O-alkylated building blocks for their construction. Due to which, in contrast to the erroneous conclusions of other studies, it has been unequivocally established that quinazolin-4-ones with alkyl halides under the classical conditions of two-phase catalysis: the solid phase (alkali metal carbonates) and liquid (aprotic solvents) are subjected to alkylation in the 3-N-position.
{"title":"N- and / or O- Alkylation of Quinazolinone Derivatives","authors":"Derenik S Khachatryan","doi":"10.19080/omcij.2020.10.555781","DOIUrl":"https://doi.org/10.19080/omcij.2020.10.555781","url":null,"abstract":"Here we report on a strategy based on the capabilities of 2D NMR spectroscopy, which focuses on determining the exact structures of promising HDAC / VEGF-2 inhibitors and intermediate N- or O-alkylated building blocks for their construction. Due to which, in contrast to the erroneous conclusions of other studies, it has been unequivocally established that quinazolin-4-ones with alkyl halides under the classical conditions of two-phase catalysis: the solid phase (alkali metal carbonates) and liquid (aprotic solvents) are subjected to alkylation in the 3-N-position.","PeriodicalId":19547,"journal":{"name":"Organic & Medicinal Chemistry International Journal","volume":"35 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-11-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74571099","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 : 2020-10-27DOI: 10.19080/OMCIJ.2020.10.555780
R. Larsson
Some of you might have heard or read about the tale of the opera singer who could really sing in tune and did so extremely well. Once she decided to try to approach the tone quality of the clink of a glass object on her table when that object was gently struck. It seemed that she succeeded, and her voice turned stronger and stronger and ----smash! --suddenly the glass object was split to pieces. The two vibration systems (the singer and the glass structure) were in harmony, as a musician would say, they were in resonance, a physicist would say.
{"title":"The Opera Diva, the Catalyst, and the Big Smash","authors":"R. Larsson","doi":"10.19080/OMCIJ.2020.10.555780","DOIUrl":"https://doi.org/10.19080/OMCIJ.2020.10.555780","url":null,"abstract":"Some of you might have heard or read about the tale of the opera singer who could really sing in tune and did so extremely well. Once she decided to try to approach the tone quality of the clink of a glass object on her table when that object was gently struck. It seemed that she succeeded, and her voice turned stronger and stronger and ----smash! --suddenly the glass object was split to pieces. The two vibration systems (the singer and the glass structure) were in harmony, as a musician would say, they were in resonance, a physicist would say.","PeriodicalId":19547,"journal":{"name":"Organic & Medicinal Chemistry International Journal","volume":"21 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-10-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79142596","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 : 2020-10-19DOI: 10.19080/omcij.2020.09.555779
Dharmawansa K V Surangi
Cancer is the second leading cause of death in global and has a major impact on human wellbeing. Recently, dietary interventions in cancer prevention and use of plant secondary metabolites in cancer therapies have been received a considerable attention. Anthocyanin, a group of flavonoids have investigated extensively for its chemopreventive and chemotherapeutic activity against the several types of cancers. Anthocyanin possess strong antioxidant activity. In addition to that, anthocyanin have shown the anti-inflammatory, anti-proliferative, apoptotic, and anti-tumorigenic properties in both in vitro and in vivo. This mini review summarizes the potential molecular mechanisms and anti-cancer activity of anthocyanin towards the breast, lung, and colorectal cancer.
{"title":"Dietary Anthocyanins- Smart Molecules with Chemo Preventive and Chemotherapeutic Activity","authors":"Dharmawansa K V Surangi ","doi":"10.19080/omcij.2020.09.555779","DOIUrl":"https://doi.org/10.19080/omcij.2020.09.555779","url":null,"abstract":"Cancer is the second leading cause of death in global and has a major impact on human wellbeing. Recently, dietary interventions in cancer prevention and use of plant secondary metabolites in cancer therapies have been received a considerable attention. Anthocyanin, a group of flavonoids have investigated extensively for its chemopreventive and chemotherapeutic activity against the several types of cancers. Anthocyanin possess strong antioxidant activity. In addition to that, anthocyanin have shown the anti-inflammatory, anti-proliferative, apoptotic, and anti-tumorigenic properties in both in vitro and in vivo. This mini review summarizes the potential molecular mechanisms and anti-cancer activity of anthocyanin towards the breast, lung, and colorectal cancer.","PeriodicalId":19547,"journal":{"name":"Organic & Medicinal Chemistry International Journal","volume":"73 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-10-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"72863831","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 : 2020-09-14DOI: 10.19080/omcij.2020.12.555776
H. Hosseinkhani
Drug delivery systems (DDS) have shown great promise in delivery of drugs and genetic materials or pharmaceuticals and other xenobiotics to their site of action within an organism and eliminate the side effect and enhance the therapeutic effects of the drugs at exact delivery position. Small interfering RNA (siRNA) is a class of nucleic acid-based drugs able to suppress gene expression by interaction with mRNA before its translation. The primary success of siRNA delivery greatly depends on suitable vectors to deliver therapeutic genes. The main problems in the delivery of siRNA-based drugs for therapeutic use are the low efficiency of siRNA delivery to target cells and tissues. This review articles discusses the recent technology of siRNA delivery systems using new biomaterials and nanoparticles. macular degeneration, diabetic macular edema, respiratory virus infection, pachyonychia congenital, hepatitis, human immunodeficiency virus infection, and cancer. There are several obstacles and concerns that should be overcome before RNAi will be used as a new therapeutic technique.
{"title":"siRNA Delivery Systems in Cancer Therapy","authors":"H. Hosseinkhani","doi":"10.19080/omcij.2020.12.555776","DOIUrl":"https://doi.org/10.19080/omcij.2020.12.555776","url":null,"abstract":"Drug delivery systems (DDS) have shown great promise in delivery of drugs and genetic materials or pharmaceuticals and other xenobiotics to their site of action within an organism and eliminate the side effect and enhance the therapeutic effects of the drugs at exact delivery position. Small interfering RNA (siRNA) is a class of nucleic acid-based drugs able to suppress gene expression by interaction with mRNA before its translation. The primary success of siRNA delivery greatly depends on suitable vectors to deliver therapeutic genes. The main problems in the delivery of siRNA-based drugs for therapeutic use are the low efficiency of siRNA delivery to target cells and tissues. This review articles discusses the recent technology of siRNA delivery systems using new biomaterials and nanoparticles. macular degeneration, diabetic macular edema, respiratory virus infection, pachyonychia congenital, hepatitis, human immunodeficiency virus infection, and cancer. There are several obstacles and concerns that should be overcome before RNAi will be used as a new therapeutic technique.","PeriodicalId":19547,"journal":{"name":"Organic & Medicinal Chemistry International Journal","volume":"39 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-09-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88130574","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 : 2020-08-18DOI: 10.19080/omcij.2020.12.555774
S. Khan
Over recent years new bioherbicides compounds from natural sources has gained much interest from the researcher’s world widely. In this study the phytotoxicity of the crude extract and its various fractions from both the stem and leaves of Acer pentapomicum (maple plant) against Lemna minor has been studied. All the fractions except aqueous extract have exhibited highly significant phytotoxicity at different concentration when compared Paraquat as a positive control. The highest herbicidal activities of 87%, was exhibited by butanol extracted samples from stem, followed by chloroform and ethyl acetate exhibiting 81% and 80% respectively. Our results confirmed that both leaves and stem extracted samples possess potent inhibitory activity against Lemna minor .
{"title":"Evaluation of In vitro Phytotoxic Activity of Medicinally Important Acer pentapomicum (Maple Plant)","authors":"S. Khan","doi":"10.19080/omcij.2020.12.555774","DOIUrl":"https://doi.org/10.19080/omcij.2020.12.555774","url":null,"abstract":"Over recent years new bioherbicides compounds from natural sources has gained much interest from the researcher’s world widely. In this study the phytotoxicity of the crude extract and its various fractions from both the stem and leaves of Acer pentapomicum (maple plant) against Lemna minor has been studied. All the fractions except aqueous extract have exhibited highly significant phytotoxicity at different concentration when compared Paraquat as a positive control. The highest herbicidal activities of 87%, was exhibited by butanol extracted samples from stem, followed by chloroform and ethyl acetate exhibiting 81% and 80% respectively. Our results confirmed that both leaves and stem extracted samples possess potent inhibitory activity against Lemna minor .","PeriodicalId":19547,"journal":{"name":"Organic & Medicinal Chemistry International Journal","volume":"357 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-08-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90291185","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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