2-Mercaptobenzimidazole Schiff Bases: Design, Synthesis, Antimicrobial Studies and Anticancer Activity on HCT-116 Cell Line

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Author(s): Sumit Tahlan, Balasubramanian Narasimhan*, Siong Meng Lim, Kalavathy Ramasamy, Vasudevan Mani, Syed Adnan Ali Shah.

Journal Name: Mini-Reviews in Medicinal Chemistry

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Background: Increased rate of mortality due to the development of resistance to currently available antimicrobial and anticancer agents initiated the need to develop new chemical entities for the treatment of microbial infections and cancer. Objective: The present study was aimed to synthesize and evaluate antimicrobial and anticancer activities of Schiff bases of 2-mercaptobenzimidazole. Method: The Schiff bases of 2-mercaptobenzimidazole were synthesized from 4-(2-(1Hbenzo[ d]imidazol-2-ylthio)acetamido)benzohydrazide. The synthesized compounds were evaluated for antimicrobial and anticancer activities by tube dilution method and sulforhodamine-B (SRB) assay, respectively. Results: Compounds 8 (MICpa, an = 2.41, 1.20 μM/ml), 10 (MICse, sa = 2.50 μM/ml), 20 (MICec = 2.34 μM/ml) and 25 (MICca = 1.46 μM/ml) showed significant antimicrobial activity against tested bacterial and fungal strains and compounds 20 (IC50 = 8 μg/ml) and 23 (IC50 = 7 μg/ml) exhibited significant anticancer activity. Conclusion: In general, the synthesized derivatives exhibited moderate antimicrobial and anticancer activity. Compounds 8 and 25 having high antifungal potential among the synthesized compounds may be taken as lead compounds for the development of novel antifungal agents.

Keywords: Antibacterial, Anticancer, Antifungal, 2-Mercaptobenzimidazole derivatives, SAR

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(E-pub Ahead of Print)
DOI: 10.2174/1389557518666181009151008
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