Bioorganic and Medicinal Chemistry Reports
A scientific open access journal in the field of Bioorganic and Medicinal Chemistry
Bioorganic and Medicinal Chemistry ReportsA scientific open access journal in the field of Bioorganic and Medicinal Chemistry
Fluorinated benzimidazole derivatives: In vitro antimicrobial activity
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.DOI http://doi.org/10.25135/bmcr.30.23.01.2692 Keywords Benzimidazole fluorine MIC antibacterial antifungal Available online: April 27, 2023 DETAILS DOWNLOAD PDF © ACG Publications. All rights reserved.