Pankaj Kumar, Abhishek Kumar, Jean Sandra Pinto, Sachin A. Kumbar, Nanditha Bhat, Prashant Nayak
Pankaj Kumar1, Abhishek Kumar1*, Jean Sandra Pinto1, Sachin A. Kumbar1, Nanditha Bhat1, Prashant Nayak2
1Department of Pharmaceutical Chemistry, NGSM Institute of Pharmaceutical Sciences, NITTE (Deemed to be University), Paneer, Deralakatte-575018, Mangaluru, Karnataka, India.
2Department of Pharmaceutics, NGSM Institute of Pharmaceutical Sciences, NITTE (Deemed to be University), Paneer, Deralakatte-575018, Mangaluru, Karnataka, India.
Volume - 15,
Issue - 4,
Year - 2022
The a,ß 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.
Cite this article:
Pankaj Kumar, Abhishek Kumar, Jean Sandra Pinto, Sachin A. Kumbar, Nanditha Bhat, Prashant Nayak. Synthesis and antimicrobial evaluation of some novel 1,5 benzodiazepine derivatives derived from pyrrolyl chalcones. Research Journal of Pharmacy and Technology. 2022; 15(4):1811-4. doi: 10.52711/0974-360X.2022.00304
Pankaj Kumar, Abhishek Kumar, Jean Sandra Pinto, Sachin A. Kumbar, Nanditha Bhat, Prashant Nayak. Synthesis and antimicrobial evaluation of some novel 1,5 benzodiazepine derivatives derived from pyrrolyl chalcones. Research Journal of Pharmacy and Technology. 2022; 15(4):1811-4. doi: 10.52711/0974-360X.2022.00304 Available on: https://rjptonline.org/AbstractView.aspx?PID=2022-15-4-70
1. Ilango SS, Remya PU, Ponnuswamy S. Synthesis, and antimicrobial activity of novel 1,5-benzodiazepines. Indian. J. Chem., 2013; 52B: 136-140.
2. De Sarro G, Gitto R, Rizzo M., Zappia M., De Sarro A. 1,4-Benzodiazepine derivatives as anticonvulsant agents in DBA/2 mice. Gen. Pharmacol.1996; 27(6):935-941. DOI: 10.1016/0306-3623(95)02147-7
3. Najafi N, Pirali M, Dowlatabadi R, Bagheri M, Rastkari N, Abdollahi M. Synthesis and analgesic and anti-inflammatory properties of new benzodiazepine derivatives. Pharmaceutical Chemistry Journal. 2005; 39(12):641-3. DOI :10.1007/s11094-006-0036-4
4. Tardibono LP, Miller MJ. Synthesis and anticancer activity of new hydroxamic acid containing 1,4 benzodiazepines. Org. Lett., 2009; 11(7):1575-1578. DOI :10.1021/ol900210h
5. Burmaoglu S, Algul O, Gobek A, Aktas AD, Ulger M. Aslan, G. Design of potent fluoro-substituted chalcones as antimicrobial agents. J. Enzyme. Inhib. Med. Chem., 2107; 32(1):490-495. DOI: 10.1080/14756366.2016.1265517
6. Hans RH, Guantai EM., Lategan C, Smith PJ, Synthesis, antimalarial and antitubercular activity of acetylenic chalcones. Bioorg. Medicinal. Chem Lett .2010; 20(3):942-944. DOI: 10.1016/j.bmcl.2009.12.062
7. Syam S, Abdelwahab SI, Al-Mamary MA, Mohan S. Synthesis of chalcones with anticancer activities. Molecules. 2012;17(6):6179-95. DOI: 10.3390/molecules17066179
8. Tavadyan LA, Manukyan ZH, Harutyunyan LH, Musayelyan MV, Sahakyan AD, Tonikyan HG. Antioxidant properties of selenophene, thiophene and their aminocarbonitrile derivatives. Antioxidants. 2017;6(2):22. DOI: 10.3390/antiox6020022
9. Nowakowsk Z. A review of anti-infective and anti-inflammatory chalcones. Eur. J. Med. Chem. 2007, 42(2):125-137. DOI: 10.1016/j.ejmech.2006.09.019
10. Kumar P, Fernandes J, Kumar A. Synthesis and Antimicrobial Evaluation of Substituted Oxazolidinones Moieties. Res. J. Pharm. Technol. 2017;10(1):98-100. DOI: 10.5958/0974-360X.2017.00023.3
11. Kumar P, Kumar A, Nayak P. Synthesis and Antimicrobial evaluation of Some novel Mercapto Pyrimidine via Pyrrole chalcone. Res. J. Pharm. Technol. 2018;11(7):2765-7. DOI: 10.5958/0974-360X.2018.00511.5