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Synthesis and Antimicrobial Evaluation of Some Novel 1,5 Benzodiazepine Derivatives Derived from Pyrrolyl Chalcones


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

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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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  • Synthesis and Antimicrobial Evaluation of Some Novel 1,5 Benzodiazepine Derivatives Derived from Pyrrolyl Chalcones

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Authors

Pankaj Kumar
Department of Pharmaceutical Chemistry, NGSM Institute of Pharmaceutical Sciences, NITTE (Deemed to be University), Paneer, Deralakatte-575018, Mangaluru, Karnataka,, India
Abhishek Kumar
Department of Pharmaceutical Chemistry, NGSM Institute of Pharmaceutical Sciences, NITTE (Deemed to be University), Paneer, Deralakatte-575018, Mangaluru, Karnataka,, India
Jean Sandra Pinto
Department of Pharmaceutical Chemistry, NGSM Institute of Pharmaceutical Sciences, NITTE (Deemed to be University), Paneer, Deralakatte-575018, Mangaluru, Karnataka,, India
Sachin A. Kumbar
Department of Pharmaceutical Chemistry, NGSM Institute of Pharmaceutical Sciences, NITTE (Deemed to be University), Paneer, Deralakatte-575018, Mangaluru, Karnataka,, India
Nanditha Bhat
Department of Pharmaceutical Chemistry, NGSM Institute of Pharmaceutical Sciences, NITTE (Deemed to be University), Paneer, Deralakatte-575018, Mangaluru, Karnataka,, India
Prashant Nayak
Department of Pharmaceutics, NGSM Institute of Pharmaceutical Sciences, NITTE (Deemed to be University), Paneer, Deralakatte-575018, Mangaluru, Karnataka,, India

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.

References