Bioorganic and Medicinal Chemistry Reports

Year: 2023 Volume: 6 Issue:January-June 1

Original Article

1) Fluorinated benzimidazole derivatives: In vitro antimicrobial activity

Bioorg. Med. Chem. Rep. (2023) 6:January-June ; 1 - 8
by Ronak Haj Ersan , Kajeen Hassan Jasim , Roaida Sadeeq , Soad Salim , Somaya Mahmood and Zina Fadhil

Given the pharmacological significance of fluorine-containing heterocycles, in the present paper, a series of benzimidazole having fluoro-benzene moiety within a single molecular framework were screened for their in vitro antimicrobial activity against some Gram-positive and Gram-negative bacteria and fungal strains. The results of antimicrobial activity demonstrated that fluoro-substituted compounds (13-15 and 17-19) have good antibacterial and antifungal properties as compared to unsubstituted parent compounds (12 and 16). Compound 18 with meta-fluoro substitution group on the phenyl ring of the side chain displayed high activity against Gram-negative bacteria with a MIC value of 31.25 μg/mL. Similarly, 2-(m-fluorophenyl)-benzimidazole derivatives 14 and 18 showed good anti-B. subtilis with a MIC value of 7.81 μg/mL. SAR studies suggested that the presence of methyl substitution group at position 5 of benzimidazole is recommended for significant antifungal activity against C. parapsilosis. The high potency suggested that compound 18 could be a starting point for further optimization to develop novel antimicrobial agents.

Benzimidazole fluorine MIC antibacterial antifungal
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