Abstract:
A series of functionalized 2-substituted benzimidazole motifs was
designed and successfully synthesized via thermal cyclization of 1,2-diaminobenzene
on COOH end of L- leucine to achieve benzimidazole derivatives 6 as the essential
precursor. The coupling of the precursor 6 with benzaldehyde derivatives a-h, ketone
series i-k, and aryl sulfonyl chlorides l-n led to the formation of the targeted 2-
substituted benzimidazole motifs 7a-n in improved yields. The targeted
benzimidazole motifs were structurally authenticated through their spectral data
and microanalytical parameters. The targeted final moieties were investigated for
potential antimicrobial activity using the agar diffusion method with gentamicin as
the clinical standard. All the compounds had a broad spectrum of activity with
compound 7k having the highest remarkable activity with MIC of 0.98 ± 0.02 μg/mL
and MBC value of 3.91 ± 0.10 μg/mL. These findings suggest that compound 7k
containing camphor might be a good candidate for the design of new antimicrobial
small-molecule drugs.
