Synthesis of some benzimidazole derivatives endowed with 1,2,3-triazole as potential inhibitors of hepatitis C virus
New derivatives of 2-thiobenzimidazole incorporating triazole moiety were synthesized, characterized and tested in vitro for antiviral activity against hepatitis C virus (HCV) and hepatitis B virus (HBV). Their cytotoxicity was determined by the reduction in the number of viable cell. All of the syn...
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| Format: | Article |
| Language: | English |
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Sciendo
2016-06-01
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| Series: | Acta Pharmaceutica |
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| Online Access: | https://doi.org/10.1515/acph-2016-0014 |
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| author | Youssif Bahaa G. M. Mohamed Yaseen A. M. Salim Mohammed T. A. Inagaki Fuyuhiko Mukai Chisato Abdu-Allah Hajjaj H. M. |
| author_facet | Youssif Bahaa G. M. Mohamed Yaseen A. M. Salim Mohammed T. A. Inagaki Fuyuhiko Mukai Chisato Abdu-Allah Hajjaj H. M. |
| author_sort | Youssif Bahaa G. M. |
| collection | DOAJ |
| description | New derivatives of 2-thiobenzimidazole incorporating triazole moiety were synthesized, characterized and tested in vitro for antiviral activity against hepatitis C virus (HCV) and hepatitis B virus (HBV). Their cytotoxicity was determined by the reduction in the number of viable cell. All of the synthesized compounds are inactive against HBV and some showed activity against HCV. In particular, two compounds showed significant activity, 2-{4-[(1-benzoylbenzimidazol-2-ylthio)methyl]-1H-1,2,3-triazol-1-yl}-N-(p-nitro-phenyl)-acetamide (13) and 2-(4-{[1-(p-chlorobenzoyl)-benzimidazol-2-ylthio)methyl]-1H-1,2,3-triazol-1-yl}-N-(p-nitrophenyl)-acetamide (17). The results give an insight into the importance of the substituent at position 2 of benzimidazole for the inhibition of HCV. |
| format | Article |
| id | doaj-art-87b458be0cf1494bbfa297731fcdb4ba |
| institution | Kabale University |
| issn | 1846-9558 |
| language | English |
| publishDate | 2016-06-01 |
| publisher | Sciendo |
| record_format | Article |
| series | Acta Pharmaceutica |
| spelling | doaj-art-87b458be0cf1494bbfa297731fcdb4ba2025-02-02T09:47:34ZengSciendoActa Pharmaceutica1846-95582016-06-0166221923110.1515/acph-2016-0014acph-2016-0014Synthesis of some benzimidazole derivatives endowed with 1,2,3-triazole as potential inhibitors of hepatitis C virusYoussif Bahaa G. M.Mohamed Yaseen A. M.0Salim Mohammed T. A.1Inagaki Fuyuhiko2Mukai Chisato3Abdu-Allah Hajjaj H. M.4 Pharmaceutical Organic Chemistry, Department, Faculty of Pharmacy, Al-Azhar University, Assiut Branch, Egypt Microbiology and Immunology, Department, Faculty of Pharmacy, Al-Azhar University, Assiut Branch, Egypt Division of Pharmaceutical Science, Graduate School of Natural Science and Technology, Kanazawa University, Kakuma-machi, Kanazawa 920-1192, Japan Division of Pharmaceutical Science, Graduate School of Natural Science and Technology, Kanazawa University, Kakuma-machi, Kanazawa 920-1192, Japan Pharmaceutical Organic Chemistry, Department, Faculty of Pharmacy, Assiut University, Assiut, 71526, EgyptNew derivatives of 2-thiobenzimidazole incorporating triazole moiety were synthesized, characterized and tested in vitro for antiviral activity against hepatitis C virus (HCV) and hepatitis B virus (HBV). Their cytotoxicity was determined by the reduction in the number of viable cell. All of the synthesized compounds are inactive against HBV and some showed activity against HCV. In particular, two compounds showed significant activity, 2-{4-[(1-benzoylbenzimidazol-2-ylthio)methyl]-1H-1,2,3-triazol-1-yl}-N-(p-nitro-phenyl)-acetamide (13) and 2-(4-{[1-(p-chlorobenzoyl)-benzimidazol-2-ylthio)methyl]-1H-1,2,3-triazol-1-yl}-N-(p-nitrophenyl)-acetamide (17). The results give an insight into the importance of the substituent at position 2 of benzimidazole for the inhibition of HCV.https://doi.org/10.1515/acph-2016-0014benzimidazoletriazoleanilideantiviralhcvhbv |
| spellingShingle | Youssif Bahaa G. M. Mohamed Yaseen A. M. Salim Mohammed T. A. Inagaki Fuyuhiko Mukai Chisato Abdu-Allah Hajjaj H. M. Synthesis of some benzimidazole derivatives endowed with 1,2,3-triazole as potential inhibitors of hepatitis C virus Acta Pharmaceutica benzimidazole triazole anilide antiviral hcv hbv |
| title | Synthesis of some benzimidazole derivatives endowed with 1,2,3-triazole as potential inhibitors of hepatitis C virus |
| title_full | Synthesis of some benzimidazole derivatives endowed with 1,2,3-triazole as potential inhibitors of hepatitis C virus |
| title_fullStr | Synthesis of some benzimidazole derivatives endowed with 1,2,3-triazole as potential inhibitors of hepatitis C virus |
| title_full_unstemmed | Synthesis of some benzimidazole derivatives endowed with 1,2,3-triazole as potential inhibitors of hepatitis C virus |
| title_short | Synthesis of some benzimidazole derivatives endowed with 1,2,3-triazole as potential inhibitors of hepatitis C virus |
| title_sort | synthesis of some benzimidazole derivatives endowed with 1 2 3 triazole as potential inhibitors of hepatitis c virus |
| topic | benzimidazole triazole anilide antiviral hcv hbv |
| url | https://doi.org/10.1515/acph-2016-0014 |
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