Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
Email: lddd@benthamscience.org


Design, Synthesis and Antimicrobial Activity of α-Aminophosphonates of Quinoline and their Molecular Docking Studies Against DNA Gyrase A

Author(s): Doddaga Srinivasulu, Muttana Vijaya Bhaskara Reddy, Donka Rajasekhar, Meriga Balaji, Chamarthi Nagaraju.


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.

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Article Details

Year: 2013
Page: [967 - 976]
Pages: 10
DOI: 10.2174/15701808113109990035
Price: $58