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

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  • El Diwani Hoda Ibrahim
    Department of Chemistry of Natural and Microbial Products, Division of Pharmaceutical and Drug Industries Research, National Research Center
  • Abdel-Mohsen Heba Tawfik
    Department of Chemistry of Natural and Microbial Products, Division of Pharmaceutical and Drug Industries Research, National Research Center
  • Salama Ismail
    Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Suez Canal University
  • Ragab Fatma Abdel-Fattah
    Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University
  • Ramla Mostafa Mahmoud
    Department of Chemistry of Natural and Microbial Products, Division of Pharmaceutical and Drug Industries Research, National Research Center
  • Galal Shadia Ahmed
    Department of Chemistry of Natural and Microbial Products, Division of Pharmaceutical and Drug Industries Research, National Research Center
  • Abdalla Mohamed Mostafa
    Research Unit, Saco Pharm. Co.
  • Abdel-Wahab Abeer
    Medical Biotechnology Department (MBD), Genetic Engineering & Biotechnology Research Institute (GEBRI), City of Scientific Research & Technology Applications
  • El Demellawy Maha Adel
    Medical Biotechnology Department (MBD), Genetic Engineering & Biotechnology Research Institute (GEBRI), City of Scientific Research & Technology Applications

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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.

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