<abstract xmlns="http://www.w3.org/1999/xhtml"><p>New derivatives of 2-thiobenzimidazole incorporating triazole moiety were synthesized, characterized and tested <italic>in vitro</italic> 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]-1<italic>H</italic>-1,2,3-triazol-1-yl}-<italic>N</italic>-(<italic>p</italic>-nitro-phenyl)-acetamide (<bold>13</bold>) and 2-(4-{[1-(<italic>p</italic>-chlorobenzoyl)-benzimidazol-2-ylthio)methyl]-1<italic>H</italic>-1,2,3-triazol-1-yl}-<italic>N</italic>-(<italic>p</italic>-nitrophenyl)-acetamide (<bold>17</bold>). The results give an insight into the importance of the substituent at position 2 of benzimidazole for the inhibition of HCV.</p></abstract>

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.

Synthesis of some benzimidazole derivatives endowed with 1,2,3-triazole as potential inhibitors of hepatitis C virus

Pharmaceutical Organic Chemistry, Department, Faculty of Pharmacy, Assiut University, Assiut, 71526, Egypt

Pharmaceutical Chemistry Department, College of Pharmacy, Al Jouf University, AlJouf Sakaka-2014, Kingdom of Saudi, Arabia

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

Acta Pharmaceutica

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

New derivatives of 2-thiobenzimidazole incorporating triazole moiety were synthesized, characterized and tested in vitro for antiviral activity against...

Synthesis of some benzimidazole derivatives endowed with 1,2,3-triazole as potential inhibitors of hepatitis C virus

Published Online: May 28, 2016

Page range: 219 - 231

Accepted: Oct 27, 2015

DOI: https://doi.org/10.1515/acph-2016-0014

Keywords
benzimidazole, triazole, anilide, antiviral, HCV, HBV

© 2016 Bahaa G. M. Youssif et al., published by De Gruyter Open

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Synthesis of some benzimidazole derivatives endowed with 1,2,3-triazole as potential inhibitors of hepatitis C virus

Published Online: May 28, 2016

Page range: 219 - 231

Accepted: Oct 27, 2015

DOI: https://doi.org/10.1515/acph-2016-0014

Keywordsbenzimidazole, triazole, anilide, antiviral, HCV, HBV

© 2016 Bahaa G. M. Youssif et al., published by De Gruyter Open

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Keywords
benzimidazole, triazole, anilide, antiviral, HCV, HBV