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
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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