Facile synthesis of N-substituted-2-(3,5-dinitrophenyl) benzimidazole derivatives for antimicrobial investigation

DAMILOLA, V. ADEROHUNMU and OLAYINKA, O. AJANI and OLAYINKA, O. TOLU-BOLAJI and OLUWATOSIN, Y. AUDU and YUXIA, ZHAO (2017) Facile synthesis of N-substituted-2-(3,5-dinitrophenyl) benzimidazole derivatives for antimicrobial investigation. In: Seventh International Conference on Advances in Applied Science and Environmental Engineering - ASEE 2017, 01-02 July, 2017, Kuala Lumpur, Malaysia.

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Abstract

Benzimidazole derivatives are crucial structural heterocyclic motifs found in diverse libraries of biologically active compounds which are therapeutically useful agents in drug discovery and medicinal research. 2-(3,5-Dinitrophenyl) benzimidazole, 1 was synthesized by [4+1]-cycloaddition of o-phenylenediamine with 3,5-dinitrobenzoic acid in catalytic amount of NH4Cl. Compound 1 was subsequently utilized as precursor which upon reaction with some halogenated molecular entity furnished the targeted N-substituted-2-(3,5-dinitrophenyl) benzimidazole derivatives in improved yields after reaction optimization engagement. The progress of reaction was monitored with TLC and the chemical structures were confirmed by analytical data and spectroscopic means such as UV, IR, mass spectra, 1H NMR, 13C NMR and DEPT-135. The titled compounds were screened for their antimicrobial activity alongside with gentamicin standard drug, using agar diffusion method while the minimum inhibitory concentration (MIC) was carried out using serial dilution method. The result showed that the synthetic method used herein was successful for the preparation of the titled benzimidazole motifs in high yields and eco-friendly manner. The compounds showed broad spectrum of activity and most of them competed favourably with gentamicin and they exhibited highly promising antibacterial potential for future drug development. They are good candidates for further studies in term of SAR study and other pharmacological screenings essential in therapeutic research.

Item Type: Conference or Workshop Item (Paper)
Uncontrolled Keywords: Antibacterial, catalysis, cyclo-addition, benzimidazole, spectroscopy, chromatography
Depositing User: Mr. John Steve
Date Deposited: 11 Mar 2019 11:31
Last Modified: 11 Mar 2019 11:31
URI: http://publications.theired.org/id/eprint/446

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