Abstract

SYNTHESIS AND IN-VITRO BIOLOGICAL EVALUATION OF BEZIMIDAZOLE DERIVATIVE

Suraj Kumar Sharma*

Abstract

Benzimidazoles are remarkably effective compounds, extensive biochemical and pharmacological studies have confirmed that these molecules are effective against various strains of microorganisms. This research is summarized to know about the chemistry of different derivatives of substituted benzimidazoles along with their pharmacological activities. Objective: Bezimidazole has a unique place in medicinal chemistry and also plays a vital role in biological processes. In the biological functions at cellular level bezimidazole plays imperative roles which lead the researchers to design a variety of its derivatives. The aim of the present study was to synthesize the novel set of N-substitutedbenzylidene-4-(1- (piperidin-1-ylmethyl)-1H-benzimidazol-2-yl)benzamine. These compounds were screened for their anti-inflammatory, anti-bacterial and anti-fungal activities. Method: A novel series of N-substitutedbenzylidene-4-(1-(piperidin-1-ylmethyl)-1H-benzimidazol-2-yl)benzamine derivatives were furnished in two steps starting from synthesis of 4-(1H-Benzimidazol-2- yl)benzamine from para-amino benzoic acid and ortho phenylene diamine then synthesis of 4-(1-(piperidin-1-ylmethyl)-1H-benzimidazol-2-yl)benzamine from 4-(1H-Benzimidazol-2- yl)benzamine formaldehyde and piperidine. Protein denaturation technique were performed for screening in vitro anti-inflammatory activity where as agar well diffusion technique was used for screening of anti-bacterial and anti-fungal activities respectively. Result: All [Nsubstitutedbenzylidene- 4-(1-(piperidin-1-ylmethyl)-1H-benzimidazol-2-yl)benzamine] the synthesized derivatives were characterized by Fourier-transform infrared spectroscopy (FTIR), 1H nuclear magnetic resonance (NMR). The result of biological screening revealed that many of the new derivatives were endowed with improved anti-inflammatory, antibacterial and anti-fungal activities. Conclusion: Nature of the substituent played a major role in anti-inflammatory, anti-microbial and anti-fungal activities. The bezimidazole derivative with hydroxyl, amino and alkoxy substitution exhibited potent anti-inflammatory anti-bacterial and anti-fungal activities. From the results, it was concluded that 4Hydroxy-3-methoxybenzaldehyde substituted benzylidene-4-(1-(piperidin-1-ylmethyl)-1H-benzimidazol-2-yl)benzamine] was the most active compound[3a].

Keywords: Bezimidazole, Substituted Aromatic Benzaldehyde, Anti-inflammatory, Anti-bacterial, anti-fungal, Agar well diffusion technique, Protein Denaturation.