Structure-based design of functionalized 2-substituted and 1,2- disubstituted benzimidazole derivatives and their in vitro antibacterial efficacy

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/m

A review on the chemistry and pharmacological properties of benzodiazepine motifs in drug design

Benzodiazepines are an important class of heterocyclic compounds in organic chemistry. They are known for their diverse physicochemical and biological properties. Some benzodiazepine derivates are well-known drugs with diverse and strong pharmacophoric moiety. An immense number of pharmacological research on benzodiazepine heterocycles and their derivatives have recently been conducted to explore its numerous pharmacological potentials as better therapeutic candidates for the treatment of various disorders, benzodiazepines, however, are one of the main sources of interest for many medicinal chemists. Researchers are drawn to the benzodiazepine nucleus for the synthesis of new drugs because of its potent pharmacophoric moiety and ring shape. Due to the emergence of new pathogenic strains’ resistance to the presently available drugs, there has been a constant demand for more effective and selective drugs. Benzodiazepine moiety has all the desired qualities for selective drug candidates used as useful therapeutic agents. Given the importance of benzodiazepine moiety, the current review aims to assess benzodiazepine syntheses as well as their pharmacological properties for potential molecular targets in therapeutic development

Structure-based design of functionalized 2-substituted and 1,2-disubstituted benzimidazole derivatives and their in vitro antibacterial efficacy

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 structure-based design of precursors 2-(1H-benzimidazol-2-yl)aniline 1, 2-(3,5-dinitro phenyl)-1H-benzimidazole 3 and 2-benzyl-1H-benzimidazole 5 were achieved by the condensation reaction of o-phenylenediamine 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 µg/mL

Heterogeneous acid catalyzed synthesis and spectroscopic characterization of Schiff bases derived from chalcone derivatives

Please read abstract in the article.Covenant Universityhttp://ejchem.journals.ekb.egam2022Chemistr