Synthesis of Certain 2-Substituted-1H-benzimidazole Derivatives as Antimicrobial and Cytotoxic Agents

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概要

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• A series of 2-substituted-1H-benzimidazole derivatives were synthesized and evaluated for antimicrobial, antifungal and cytotoxic activities. The results showed that all tested compounds showed potent antimicrobial activity against some species of Gram-negative bacteria (Pseudomonas aeruginosa, Escherichia coli, Salmonella typhi) and fungi (Candida albicans) with minimum inhibitory concentrations (MICs) lower than 0.016 µg/mL. In contrast, all tested compounds were inactive against Staphylococcus aureus (Gram-positive bacterium). The final targets were also tested for their antitumor activity in vitro on cervical carcinoma (HeLa) cell line. Eight of the test compounds displayed more potent cytotoxic effect than doxorubicin at nanomolar concentrations. Compounds 2c and 3c exerted the strongest cytoyoxic effect with IC50 15 and 13 nM, respectively.

著者

• Ragab Yasser

  Department of Microbiology and Immunology, Faculty of Pharmacy, Cairo University

• Ahmed Eman

  Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Cairo University

• Khalil Nadia

  Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Cairo University

• Taher Azza

  Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Cairo University

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