Synthesis and antimicrobial evaluation of some novel 1,5 benzodiazepine derivatives derived from pyrrolyl chalcones Kumar Pankaj1, Kumar Abhishek1,*, Pinto Jean Sandra1, Kumbar Sachin A.1, Bhat Nanditha1, Nayak Prashant2 1Department of Pharmaceutical Chemistry, NGSM Institute of Pharmaceutical Sciences, NITTE (Deemed to be University), Paneer, Deralakatte-575018, Mangalore, Karnataka, India 2Department of Pharmaceutics, NGSM Institute of Pharmaceutical Sciences, NITTE (Deemed to be University), Paneer, Deralakatte-575018, Mangalore, Karnataka, India *Corresponding Author E-mail: abhi12bunty@gmail.com
Online Published on 08 June, 2022. Abstract The a,P unsaturated ketone 3-(2,4-dimethyl-lH-pyrrol-3-yl)-l-phenylprop-2-en-l-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. Top Keywords Benzodiazepines, Antimicrobial, Docking, Topoisomerases, O-Phenylenediamine. Top |