Synthesis, Molecular Modeling, and Biological Evaluation of Novel Benzimidazole Derivatives as Inhibitors of Hepatitis C Virus RNA Replication

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概要

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• In this study, synthesis and docking studies of a series of new benzimidazole derivatives linked to substituted pyrimidines either through the methylenethio linkage or its bioisosteric methylene amino bridge were carried out. All the synthesized compounds were evaluated for their hepatitis C virus (HCV) RNA replication-inhibitory activity. Compounds 4d, 4f, and 4h were found to be more potent than VX-950 (IC50/90 of 4d=0.123/0.321, 4f=0.145/0.345, 4h=0.129/0.432, VX-950=0.20/0.45 µM, respectively) and 6d (IC50/90=0.116/0.452 µM) displayed activity very similar to that of the standard. Compounds 4d, 4f, 4h, and 6d were potent HCV RNA replication inhibitors and are good drug candidates for further investigations.

• 公益社団法人 日本薬学会の論文

著者

• Ragab Fatma

  Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University

• Abdalla Mohamed

  Research Unit, Univet Pharmaceutical Co.

• Salama Ismail

  Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Suez Canal University

• Abdel-Wahab Abeer

  Medical Biotechnology Department (MBD), Genetic Engineering & Biotechnology Research Institute (GEBRI), City of Scientific Research & Technology Applications

• El Diwani

  Department of Chemistry of Natural and Microbial Products, Division of Pharmaceutical and Drug Industries Research, National Research Center

• Abdel-Mohsen Heba

  Department of Chemistry of Natural and Microbial Products, Division of Pharmaceutical and Drug Industries Research, National Research Center

• Ramla Mostafa

  Department of Chemistry of Natural and Microbial Products, Division of Pharmaceutical and Drug Industries Research, National Research Center

• Galal Shadia

  Department of Chemistry of Natural and Microbial Products, Division of Pharmaceutical and Drug Industries Research, National Research Center

• El Demellawy

  Medical Biotechnology Department (MBD), Genetic Engineering & Biotechnology Research Institute (GEBRI), City of Scientific Research & Technology Applications

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