Ajani, Olayinka O. and Tolu-Bolaji, Olayinka O. and Olorunshola, S. J. and Zhao, Yuxia and Aderohunmu, D. V. (2017) Structure-based design of functionalized 2-substituted and 1,2- disubstituted benzimidazole derivatives and their in vitro antibacterial efficacy. Journal of Advanced Research, 8. pp. 703-712.
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Abstract
The aim of this present study was to synthesize 2-substituted and 1,2-disubstituted benzimidazole derivatives to investigate their antibacterial diversity for possible future drug design. The structurebased design of precursors 2-(1H-benzimidazol-2-yl)aniline 1, 2-(3,5-dinitro phenyl)-1Hbenzimidazole 3 and 2-benzyl-1H-benzimidazole 5 were achieved by the condensation reaction of ophenylenediamine with anthranilic acid, 3,5-dinitrophenylbenzoic acid, and phenylacetic acid, respectively. The precursors 1, 3 and 5, upon reaction with six different electrophile-releasing agents, furnished the corresponding 2-substituted benzimidazole, 2a-f and 1,2-disubstituted benzimidazole derivatives 4a-f and 6a-f, respectively. The structural identity of the targeted compounds was authenticated by elemental analytical data and spectral information from FT-IR, UV, 1H, and 13C NMR. The outcome of the findings from the in vitro screening unveiled 2-benzyl-1-(phenylsulfonyl)-1H-benzimidazole 6b as the most active derivative with lowest MIC value of 15.63 mg/mL
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | Benzimidazole Antibacterial Activity index Cycloaddition Spectroscopy |
| Subjects: | Q Science > Q Science (General) Q Science > QD Chemistry |
| Divisions: | Faculty of Engineering, Science and Mathematics > School of Chemistry |
| Depositing User: | Mrs Hannah Akinwumi |
| Date Deposited: | 22 Mar 2019 07:48 |
| Last Modified: | 22 Mar 2019 07:48 |
| URI: | http://eprints.covenantuniversity.edu.ng/id/eprint/12515 |
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