Informatics Publishing Limited

Pankaj Kumar ¹, Abhishek Kumar ¹, Jean Sandra Pinto ¹, Sachin A. Kumbar ¹, Nanditha Bhat ¹, Prashant Nayak ²

Affiliations
1 Department of Pharmaceutical Chemistry, NGSM Institute of Pharmaceutical Sciences, NITTE (Deemed to be University), Paneer, Deralakatte-575018, Mangaluru, Karnataka,, IN
2 Department of Pharmaceutics, NGSM Institute of Pharmaceutical Sciences, NITTE (Deemed to be University), Paneer, Deralakatte-575018, Mangaluru, Karnataka,, IN

Abstract

The α,β unsaturated ketone 3-(2,4-dimethyl-1H-pyrrol-3-yl)-1-phenylprop-2-en-1-onederivatives were treated with benzene-1,2-diamine to obtain 2-(2,4-dimethyl-1H-pyrrol-3-yl)-4-phenyl-2,3-dihydro-1H-benzo[b][1,4]diazepine derivatives. These synthesized compound were characterized by IR, 1H NMR, and mass spectroscopy. These synthesized molecules were evaluated for invitro antimicrobial activity. All The synthesized compounds, showed potent anti-microbial activity as compare to reference drug. In these study the synthesized were docked with Type IIA topoisomerases 2XCT using glide dock program and binding affinity were predicted for the synthesized compounds. The compound AP8 and AP9 have shown more active as per binding energy.

Keywords

Benzodiazepines, Antimicrobial, Docking, Topoisomerases, o-Phenylenediamine.

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