Abstract
A new series of diethyl (substituted phenyl/thiophen-2-yl)(quinolin-8-ylamino)methylphosphonates 4a-j of biological interest was synthesized by Kabachnik-Fields reaction. The title compounds were screened for their antimicrobial activity. Some of the compounds in the series exhibited promising antibacterial and antifungal activity. The newly synthesized compounds were subjected to molecular docking studies for the inhibition of the enzyme DNA Gyrase A, which is a new target for microbes (E. coli). The docking studies shown that 4b, 4c, 4e, 4g and 4h posses the highest binding energies compared to ciprofloxacin.
Keywords: α-Aminophosphonates, Antibacterial activity, Antifungal activity, CeCl3.7H2O, Molecular docking.
Letters in Drug Design & Discovery
Title:Design, Synthesis and Antimicrobial Activity of α-Aminophosphonates of Quinoline and their Molecular Docking Studies Against DNA Gyrase A
Volume: 10 Issue: 10
Author(s): Doddaga Srinivasulu, Muttana Vijaya Bhaskara Reddy, Donka Rajasekhar, Meriga Balaji and Chamarthi Nagaraju
Affiliation:
Keywords: α-Aminophosphonates, Antibacterial activity, Antifungal activity, CeCl3.7H2O, Molecular docking.
Abstract: A new series of diethyl (substituted phenyl/thiophen-2-yl)(quinolin-8-ylamino)methylphosphonates 4a-j of biological interest was synthesized by Kabachnik-Fields reaction. The title compounds were screened for their antimicrobial activity. Some of the compounds in the series exhibited promising antibacterial and antifungal activity. The newly synthesized compounds were subjected to molecular docking studies for the inhibition of the enzyme DNA Gyrase A, which is a new target for microbes (E. coli). The docking studies shown that 4b, 4c, 4e, 4g and 4h posses the highest binding energies compared to ciprofloxacin.
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Srinivasulu Doddaga, Vijaya Bhaskara Reddy Muttana, Rajasekhar Donka, Balaji Meriga and Nagaraju Chamarthi, Design, Synthesis and Antimicrobial Activity of α-Aminophosphonates of Quinoline and their Molecular Docking Studies Against DNA Gyrase A, Letters in Drug Design & Discovery 2013; 10 (10) . https://dx.doi.org/10.2174/15701808113109990035
DOI https://dx.doi.org/10.2174/15701808113109990035 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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