Ajani, Olayinka OyewaleJoseph, Olaoluwasubomi EneyemeIyaye, King TamunodikibugerereOctober, NatashaAderohunmu, Damilola VictoriaOlorunshola, Shade JohnAudu, Oluwatosin Yemisi2021-07-292021-07-292020Ajani, O.O., Joseph, O.E., Iya, K.T. et al. 2020, 'Facile synthesis, characterization and in vitro antibacterial efficacy of functionalized 2-substituted benzimidazole motifs', Indonesian Journal of Chemistry, vol. 20, no. 1. pp. 72 - 87.14119420 (print)2460-1578 (online)10.22146/ijc.40448http://hdl.handle.net/2263/81057A 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.en© 2021 Indonesian Journal of Chemistry. This work is licensed under a Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International License.Benzimidazole[4+1]-cycloadditionSerial dilutionSAR studyAntibacterialStructure activity relationship (SAR)Article