{"title":"噻吩-2- carboxamide的恶二唑基、吡唑基和噻唑基衍生物抗菌和抗hcv药物的合成。","authors":"Ola H Rizk, Omaima G Shaaban, Abeer E Abdel Wahab","doi":"10.2174/1874104501711010038","DOIUrl":null,"url":null,"abstract":"<p><strong>Introduction: </strong>Three series of pyrazole, thiazole and 1,3,4-oxadiazole, derivatives were synthesized starting from 5-amino-4-(hydrazinocarbonyl)-3-methylthiophene-2-carboxamide <b>(2)</b>.</p><p><strong>Methods: </strong>All compounds were investigated for their preliminary antimicrobial activity. They were proved to exhibit remarkable antimicrobial activity against <i>Pseudomonas aeruginosa</i> with insignificant activity towards Gram positive bacterial strains and fungi.</p><p><strong>Results: </strong><i>In-vitro</i> testing of the new compounds on hepatitis-C virus (HCV) replication in hepatocellular carcinoma cell line HepG2 infected with the virus utilizing the reverse transcription polymerase chain reaction technique (RT-PCR) generally showed inhibition of the replication of HCV RNA (-) strands at low concentration, while, eight compounds; <b>3a</b>, <b>6</b>, <b>7a</b>, <b>7b</b>, <b>9a</b>, <b>9b</b>, <b>10a</b> and <b>11b</b> proved to inhibit the replication of HCV RNA (+) and (-) strands at very low concentration range 0.08-0.36 μg/mL.</p><p><strong>Conclusion: </strong>Compounds <b>7b</b> and <b>11b</b> displayed the highest anti-HCV and antimicrobial activities in this study.</p>","PeriodicalId":39133,"journal":{"name":"Open Medicinal Chemistry Journal","volume":"11 ","pages":"38-53"},"PeriodicalIF":0.0000,"publicationDate":"2017-04-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.2174/1874104501711010038","citationCount":"7","resultStr":"{\"title\":\"Synthesis of Oxadiazolyl, Pyrazolyl and Thiazolyl Derivatives of Thiophene-2-Carboxamide as Antimicrobial and Anti-HCV Agents.\",\"authors\":\"Ola H Rizk, Omaima G Shaaban, Abeer E Abdel Wahab\",\"doi\":\"10.2174/1874104501711010038\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><strong>Introduction: </strong>Three series of pyrazole, thiazole and 1,3,4-oxadiazole, derivatives were synthesized starting from 5-amino-4-(hydrazinocarbonyl)-3-methylthiophene-2-carboxamide <b>(2)</b>.</p><p><strong>Methods: </strong>All compounds were investigated for their preliminary antimicrobial activity. They were proved to exhibit remarkable antimicrobial activity against <i>Pseudomonas aeruginosa</i> with insignificant activity towards Gram positive bacterial strains and fungi.</p><p><strong>Results: </strong><i>In-vitro</i> testing of the new compounds on hepatitis-C virus (HCV) replication in hepatocellular carcinoma cell line HepG2 infected with the virus utilizing the reverse transcription polymerase chain reaction technique (RT-PCR) generally showed inhibition of the replication of HCV RNA (-) strands at low concentration, while, eight compounds; <b>3a</b>, <b>6</b>, <b>7a</b>, <b>7b</b>, <b>9a</b>, <b>9b</b>, <b>10a</b> and <b>11b</b> proved to inhibit the replication of HCV RNA (+) and (-) strands at very low concentration range 0.08-0.36 μg/mL.</p><p><strong>Conclusion: </strong>Compounds <b>7b</b> and <b>11b</b> displayed the highest anti-HCV and antimicrobial activities in this study.</p>\",\"PeriodicalId\":39133,\"journal\":{\"name\":\"Open Medicinal Chemistry Journal\",\"volume\":\"11 \",\"pages\":\"38-53\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2017-04-28\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.2174/1874104501711010038\",\"citationCount\":\"7\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Open Medicinal Chemistry Journal\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.2174/1874104501711010038\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2017/1/1 0:00:00\",\"PubModel\":\"eCollection\",\"JCR\":\"Q2\",\"JCRName\":\"Pharmacology, Toxicology and Pharmaceutics\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Open Medicinal Chemistry Journal","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.2174/1874104501711010038","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2017/1/1 0:00:00","PubModel":"eCollection","JCR":"Q2","JCRName":"Pharmacology, Toxicology and Pharmaceutics","Score":null,"Total":0}
Synthesis of Oxadiazolyl, Pyrazolyl and Thiazolyl Derivatives of Thiophene-2-Carboxamide as Antimicrobial and Anti-HCV Agents.
Introduction: Three series of pyrazole, thiazole and 1,3,4-oxadiazole, derivatives were synthesized starting from 5-amino-4-(hydrazinocarbonyl)-3-methylthiophene-2-carboxamide (2).
Methods: All compounds were investigated for their preliminary antimicrobial activity. They were proved to exhibit remarkable antimicrobial activity against Pseudomonas aeruginosa with insignificant activity towards Gram positive bacterial strains and fungi.
Results: In-vitro testing of the new compounds on hepatitis-C virus (HCV) replication in hepatocellular carcinoma cell line HepG2 infected with the virus utilizing the reverse transcription polymerase chain reaction technique (RT-PCR) generally showed inhibition of the replication of HCV RNA (-) strands at low concentration, while, eight compounds; 3a, 6, 7a, 7b, 9a, 9b, 10a and 11b proved to inhibit the replication of HCV RNA (+) and (-) strands at very low concentration range 0.08-0.36 μg/mL.
Conclusion: Compounds 7b and 11b displayed the highest anti-HCV and antimicrobial activities in this study.
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