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Asian Journal of Organic & Medicinal Chemistry最新文献

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Synthesis of Thienyl-Isoxazolines and in vitro Screening for their Antimicrobial Activity 噻吩基异恶唑啉类化合物的合成及体外抗菌活性筛选
Asian Journal of Organic & Medicinal Chemistry Pub Date : 2020-01-01 DOI: 10.14233/ajomc.2020.ajomc-p277
C. B. Vagish, N. Renuka, K. Kumar, H. Jayadevappa
{"title":"Synthesis of Thienyl-Isoxazolines and in vitro Screening for their Antimicrobial Activity","authors":"C. B. Vagish, N. Renuka, K. Kumar, H. Jayadevappa","doi":"10.14233/ajomc.2020.ajomc-p277","DOIUrl":"https://doi.org/10.14233/ajomc.2020.ajomc-p277","url":null,"abstract":"A series of thiophene conjugated isoxazoles were efficiently synthesized using a recyclable heterogeneous catalyst Amberlyst-15 in good yields. The synthesized new compounds 5(a-j) were characterized by spectral and elemental analysis and screened in vitro for their antimicrobial potencies. Amongst the synthesized series; compounds 5c and 5j having chloro substitution on both thiophene and aromatic ring exhibited excellent inhibition against the tested species","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78723509","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}
引用次数: 2
Catalyst and Solvent Free Synthesis and Biological Activities of Imidazo[1,2-a]pyridine 咪唑[1,2-a]吡啶的无溶剂合成及生物活性研究
Asian Journal of Organic & Medicinal Chemistry Pub Date : 2020-01-01 DOI: 10.14233/ajomc.2020.ajomc-p283
G. B. Gundlewad, S. Wagh, B. R. Patil
{"title":"Catalyst and Solvent Free Synthesis and Biological Activities of Imidazo[1,2-a]pyridine","authors":"G. B. Gundlewad, S. Wagh, B. R. Patil","doi":"10.14233/ajomc.2020.ajomc-p283","DOIUrl":"https://doi.org/10.14233/ajomc.2020.ajomc-p283","url":null,"abstract":"A series of imidazo[1,2-a]pyridines were synthesized by the reaction of α-chloroacetophenone and 2- aminopyridine under catalyst and solvent free condition. The synthesized compounds were characterized by IR, 1H NMR, 13C NMR and mass spectral data. These imidazo[1,2-a]pyridines were screened for antiinflammatory activity by carrageenan induced rat hind paw edema model. Good anti-inflammatory activity was shown by few compounds. The antibacterial activity was studied against two Grampositive bacteria S. aureus and B. subtilis, two Gram-negative bacteria E. coli and S. typhi and antifungal activity against P. chrysogenum, F. moneliforme, A. flavus and A. niger. All the synthesized compounds were desplayed good antimicrobial and antifungal activities. Some of the compounds were shown higher antibacterial activity than reference drug penicillin.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"326 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79719308","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}
引用次数: 1
Molecular Docking Studies of Some Natural Products AgainstSARS-CoV-2 Main Protease: Potential Therapeutic Agents for COVID-19 部分抗sars - cov -2主蛋白酶天然产物与新冠病毒潜在治疗剂的分子对接研究
Asian Journal of Organic & Medicinal Chemistry Pub Date : 2020-01-01 DOI: 10.14233/ajomc.2020.ajomc-p288
Gnanavel Sadhasivam
{"title":"Molecular Docking Studies of Some Natural Products Against\u0000SARS-CoV-2 Main Protease: Potential Therapeutic Agents for COVID-19","authors":"Gnanavel Sadhasivam","doi":"10.14233/ajomc.2020.ajomc-p288","DOIUrl":"https://doi.org/10.14233/ajomc.2020.ajomc-p288","url":null,"abstract":"The severe form of respiratory disease (COVID-19), caused by SARS-COV-2 virus, has evolved into a pandemic is the defining global health crisis of our time and greatest challenge we have faced since second World War. Hence, the current situation demands an immediate need to explore all the possible therapeutic strategies that can be control spread of the diseases. We identified potent COVID-19 Mpro inhibitors based on molecular docking studies on 24 known antiviral natural compounds, which are from medicinal plants and marine sponges. The results revealed that 15 potential COVID-19 main protease inhibitors have been identified among the 24 natural compounds of plants and marine origin. The result further revealed that the selected natural products that has lower free binding energy is Halituline (-8.41 Kcal/mol). As these active compounds were extensively validated by molecular docking, the chance that at least few of these compounds could be bioactive is excellent.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"28 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84212910","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}
引用次数: 0
Stability Indicating RP-UPLC Photo-Diode Array basedMethod for Determination of Edoxaban Tosylate 稳定性指示RP-UPLC光电二极管阵列测定Tosylate依多沙班的方法
Asian Journal of Organic & Medicinal Chemistry Pub Date : 2020-01-01 DOI: 10.14233/ajomc.2020.ajomc-p270
D. Patel, B. Rana, S. Maru, A. Vyas, A. Patel, A.I. Patel, N. K. Patel
{"title":"Stability Indicating RP-UPLC Photo-Diode Array based\u0000Method for Determination of Edoxaban Tosylate","authors":"D. Patel, B. Rana, S. Maru, A. Vyas, A. Patel, A.I. Patel, N. K. Patel","doi":"10.14233/ajomc.2020.ajomc-p270","DOIUrl":"https://doi.org/10.14233/ajomc.2020.ajomc-p270","url":null,"abstract":"The objective of the current study was to develop a specific, precise, accurate and robust gradient stability indicating reversed-phase ultra performance liquid chromatography (RP-UPLC-PDA) assay method and validated for determination of edoxaban tosylate in API. Gradient separation was achieved on an acquity UPLC BEH C18 column (50 mm, 2.1 mm and 1.7 μm) column using mobile phase of acetoitrile:20 mM potassium dihydrogen phosphate, pH 3.0 ± 0.05 adjust with OPA at flow rate of 0.6 mL/min, the injection volume was 1 μL and the detection was carried out of 289 nm by using photodiode array detector. The drug was subjected to oxidation, hydrolysis, photolysis, and heat to apply stress condition. The method was linear in the drug concentration range of 100-300 μg/mL with correlation coefficient of 0.999. Degradation products produced as a result of stress studies did not interfere with detection of edoxaban tosylate and the assay, thus developed stability indicating method can be used for routine analysis in pharmaceutical industry.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"10 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91339032","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}
引用次数: 1
The Chemical Sciences' Advances on Coronavirus Disease 2019 (COVID-19) 2019冠状病毒病(COVID-19)化学研究进展
Asian Journal of Organic & Medicinal Chemistry Pub Date : 2020-01-01 DOI: 10.14233/ajomc.2020.ajomc-p286
Shovan Mondal
{"title":"The Chemical Sciences' Advances on Coronavirus Disease 2019 (COVID-19)","authors":"Shovan Mondal","doi":"10.14233/ajomc.2020.ajomc-p286","DOIUrl":"https://doi.org/10.14233/ajomc.2020.ajomc-p286","url":null,"abstract":"The novel β-coronavirus (SARS-CoV-2) causes coronavirus disease (COVID-19), which is presently a pandemic affecting numerous nations worldwide including a grim fatality of over 9 lakhs deaths till August, 2020. But even after the 9 months of the outbreak of this deadly disease, there is no particular medication or vaccine so far that can be recommended for the treatment of COVID-19 patients. Therefore, chemists are struggling to understand and dissect the viral structure of this SARS-CoV-2, unwind its pathogenesis and pinpoint its vaccines and therapies as well. In this current study, the author endeavor to sum up the ongoing advances of chemical sciences about COVID-19 focusing mainly on the developments of its therapeutics.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"38 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86644852","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}
引用次数: 0
RP-UPLC Stability Indicating Assay Method for Simultaneous Estimation ofDextromethorphan Hydrobromide and Chlorpheniramine Maleate in Tablet Dosage Form RP-UPLC稳定性指示法同时测定片剂中氢溴酸右美沙芬和马来酸氯苯那敏的含量
Asian Journal of Organic & Medicinal Chemistry Pub Date : 2020-01-01 DOI: 10.14233/ajomc.2020.ajomc-p269
A. Patel, Nishith K. Patel, A. Vyas, A.B. Patel, A.I. Patel
{"title":"RP-UPLC Stability Indicating Assay Method for Simultaneous Estimation of\u0000Dextromethorphan Hydrobromide and Chlorpheniramine Maleate in Tablet Dosage Form","authors":"A. Patel, Nishith K. Patel, A. Vyas, A.B. Patel, A.I. Patel","doi":"10.14233/ajomc.2020.ajomc-p269","DOIUrl":"https://doi.org/10.14233/ajomc.2020.ajomc-p269","url":null,"abstract":"RP-UPLC method was developed and validated for the determination of chlorpheniramine maleate and dextromethorphan hydrobromide in tablet dosage form. Reverse phase waters acquity UPLC BEH C18 (50 mm × 2.1 mm, 1.7 μm) column using isocratic mobile phase of 0.5 mL 0.1% TFA (trifluroacetic acid) in H2O:CH3CN (70:30 %v/v). The flow rate was 0.2 mL/min and 252 nm wavelength use for detection on PDA detector. The retention time of chlorpheniramine maleate was 1.2 min and 2.2 min for dextromethorphan hydrobromide. Chlorpheniramine maleate and dextromethorphan hydrobromide was subjected to stress conditions including acidic, alkaline, oxidation, photolysis and thermal degradation. The method was validated as per ICH guideline with respect to samples to specificity, precision, accuracy, linearity and robustness.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88195655","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}
引用次数: 0
Synthesis of Some New 5-Indolylidene-4-thiazolidinone Derivatives of1,2,4-triazole as Potent Antioxidant and Antifungal Agents 新型1,2,4-三唑类5-吲哚吡啶-4-噻唑烷酮衍生物的合成
Asian Journal of Organic & Medicinal Chemistry Pub Date : 2019-10-12 DOI: 10.14233/ajomc.2019.ajomc-p214
T. Khan, R. Yadav
{"title":"Synthesis of Some New 5-Indolylidene-4-thiazolidinone Derivatives of\u00001,2,4-triazole as Potent Antioxidant and Antifungal Agents","authors":"T. Khan, R. Yadav","doi":"10.14233/ajomc.2019.ajomc-p214","DOIUrl":"https://doi.org/10.14233/ajomc.2019.ajomc-p214","url":null,"abstract":"A series of 1,2,4-triazolyl-4-(5-indolylidene)-thiazolidinone derivatives were synthesized and screened\u0000for their antifungal and antioxidant activity. Among these synthesized compounds 3d, 3g showing\u0000good antifungal activity and compounds 3b, 3d, 3f and 3h have high % antioxidant activity with lower\u0000IC50 value of 11.21, 20.89, 17.51 and 14.05 respectively. We report the antioxidant potential of the said\u0000class of compound in which free radical is generated by methelenic and 2nd carbon of thiazolidinone\u0000ring. The antifungal activity reported against A. niger, C. albicans and A. flavus. The antioxidant\u0000activity of all the synthesized compounds was screened by H2O2, DPPH scavenging and by\u0000phosphomolybdenum method with respect to ascorbic acid.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"305 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-10-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79823281","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}
引用次数: 0
Facile Synthesis and Biological Evaluation of Cyclopropyl-PyrazoleHybrids in [bmim][PF6]-Water Biphasic System as Antifungal Agents [bmim][PF6]-水双相体系中环丙基吡唑杂合物的快速合成及生物学评价
Asian Journal of Organic & Medicinal Chemistry Pub Date : 2019-10-12 DOI: 10.14233/ajomc.2019.ajomc-p192
P. C. Burde, A. Rahatgaonkar
{"title":"Facile Synthesis and Biological Evaluation of Cyclopropyl-Pyrazole\u0000Hybrids in [bmim][PF6]-Water Biphasic System as Antifungal Agents","authors":"P. C. Burde, A. Rahatgaonkar","doi":"10.14233/ajomc.2019.ajomc-p192","DOIUrl":"https://doi.org/10.14233/ajomc.2019.ajomc-p192","url":null,"abstract":"3-Cyclopropyl-5-(4-substituted)-1-phenyl-4,5-dihydro-1H-pyrazoles derived from corresponding\u0000chalcones were synthesized and evaluated for their biological activities. A convenient synthesis of a\u0000library of these compounds in 1-butyl-3-methylimidazolium hexafluorophosphate-water biphasic system\u0000at ambient temperature has been accomplished. The ionic liquid, [bmim][PF6] and water which are\u0000immiscible, has been easily recycled and reused after separation of the products without any noticeable\u0000diminution in its activity.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"16 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-10-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79958835","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}
引用次数: 0
Origination Progress and Utility of Selective Estrogen Receptor Modulators in ClinicalPractice as an Efficient Substitute of Estrogen for Treating Hormone Dependent Issues 选择性雌激素受体调节剂作为雌激素的有效替代品治疗激素依赖的起源、进展及临床应用
Asian Journal of Organic & Medicinal Chemistry Pub Date : 2019-10-12 DOI: 10.14233/ajomc.2019.ajomc-p188
A. Kulshrestha, J. Pandey
{"title":"Origination Progress and Utility of Selective Estrogen Receptor Modulators in Clinical\u0000Practice as an Efficient Substitute of Estrogen for Treating Hormone Dependent Issues","authors":"A. Kulshrestha, J. Pandey","doi":"10.14233/ajomc.2019.ajomc-p188","DOIUrl":"https://doi.org/10.14233/ajomc.2019.ajomc-p188","url":null,"abstract":"The discovery, development and utility of selective estrogen receptor modulators (SERMs) are presented\u0000in this study. As per literature review SERMs used in the treatment of estrogen hormone responsive\u0000diseases like osteoporosis, Alzheimer, angiogenesis, hyperlipidemia, coronary heart disease,\u0000atherosclerosis, endometriosis, breast cancer, post-menopausal depression, dysfunctional uterine\u0000bleeding, gynacomastia, Albright syndrome, ovarian cancer, dyspareunia, cyclical mastalgia,\u0000hypogondism and induced ovulation in sub-fertile woman, etc. Basically world wide a large no.\u0000compounds available those function as SERMs successfully or under different phase clinical trials or\u0000discontinued because of unwanted side effects during clinical trials. This work describes the specific\u0000reference compounds which have created a substitute of estrogen for treating hormone dependent\u0000issues.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"20 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-10-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78647023","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}
引用次数: 0
Synthesis, Characterization and Biological Activities of Substituted1-[Benzothiazol-(1H)-2-yl]-3-phenyl-prop-2-en-1-ones 取代1-[苯并噻唑-(1H)-2-基]-3-苯基-丙-2-烯-1的合成、表征及生物活性
Asian Journal of Organic & Medicinal Chemistry Pub Date : 2019-10-12 DOI: 10.14233/ajomc.2019.ajomc-p181
C. Anuba, T. Reji
{"title":"Synthesis, Characterization and Biological Activities of Substituted\u00001-[Benzothiazol-(1H)-2-yl]-3-phenyl-prop-2-en-1-ones","authors":"C. Anuba, T. Reji","doi":"10.14233/ajomc.2019.ajomc-p181","DOIUrl":"https://doi.org/10.14233/ajomc.2019.ajomc-p181","url":null,"abstract":"A series of ortho and para substituted 1-[benzothiazol-(1H)-2-yl]-3-phenyl-prop-2-en-1-one derivatives\u0000were synthesized from 2-acetyl benzothiazole and ortho and para-substituted benzaldehye using ethanol\u0000as solvent. The synthesized compounds were characterized by UV-visible, FT-IR, 1H NMR and mass\u0000spectrometry. Antioxidant activities of synthesized compounds have been evaluated by DPPH free\u0000radical scavenging activity using ascorbic acid as standard. The standard solution and 1-[benzothiazol-\u0000(1H)-2-yl]-3-phenylprop-2-en-1-ones compounds were prepared with different concentrations.\u0000Anticancer activity of 1-[benzothiazol-(1H)-2-yl]-3-phenylprop-2-en-1-one and 1-[benzothiazol-(1H)-\u00002-yl]-3(4-chlorophenyl)prop-2-en-1-one were assigned by MTT assays.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"8 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-10-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88788744","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}
引用次数: 0
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