Abstract
In search for the new antimicrobial agents owing to drug resistant bacteria and fungi, a series of rationally designed aza analogs of flavones has been designed and synthesized. The design of the analogs involved incorporation of quinolone nucleus within the flavone framework keeping in view the antimicrobial potential of both the classes. The series of compounds was evaluated for the antibacterial and antifungal activity against 3 Gram negative bacterial strains; E. coli (MTCC 82), S. typhi (MTCC 1251), P. aeruginosa (MTCC 2642), 2 gram positive bacterial strains B. subtilis (MTCC 2451), S. aureus (MTCC 96) and 2 pathogenic fungal strains, C. albicans (MTCC 3018), C. tropicalis (MTCC). The results of the antimicrobial evaluation clearly indicated the influence of the electronic factors linked with the aryl ring at the 2nd position with compounds bearing methoxy substitutents exhibiting significant antimicrobial profile as compared to the compounds bearing deactivating groups. The influence of placement of bicyclic, heteroaryl and bicyclic heteroaryl ring at the 2nd position of the analogs was also observed.
Keywords: Flavones, Quinolones, Antimicrobial activity, Strains, Antibacterial, Antifungal
Letters in Drug Design & Discovery
Title:Aza Analogs of Flavones as Potential Antimicrobial Agents
Volume: 10 Issue: 4
Author(s): Sahil Sharma, Vikas Thakur, Ritu Ojha, Abhishek Budhiraja, Kunal Nepali and Preet Mohinder Singh Bedi
Affiliation:
Keywords: Flavones, Quinolones, Antimicrobial activity, Strains, Antibacterial, Antifungal
Abstract: In search for the new antimicrobial agents owing to drug resistant bacteria and fungi, a series of rationally designed aza analogs of flavones has been designed and synthesized. The design of the analogs involved incorporation of quinolone nucleus within the flavone framework keeping in view the antimicrobial potential of both the classes. The series of compounds was evaluated for the antibacterial and antifungal activity against 3 Gram negative bacterial strains; E. coli (MTCC 82), S. typhi (MTCC 1251), P. aeruginosa (MTCC 2642), 2 gram positive bacterial strains B. subtilis (MTCC 2451), S. aureus (MTCC 96) and 2 pathogenic fungal strains, C. albicans (MTCC 3018), C. tropicalis (MTCC). The results of the antimicrobial evaluation clearly indicated the influence of the electronic factors linked with the aryl ring at the 2nd position with compounds bearing methoxy substitutents exhibiting significant antimicrobial profile as compared to the compounds bearing deactivating groups. The influence of placement of bicyclic, heteroaryl and bicyclic heteroaryl ring at the 2nd position of the analogs was also observed.
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Sharma Sahil, Thakur Vikas, Ojha Ritu, Budhiraja Abhishek, Nepali Kunal and Mohinder Singh Bedi Preet, Aza Analogs of Flavones as Potential Antimicrobial Agents, Letters in Drug Design & Discovery 2013; 10 (4) . https://dx.doi.org/10.2174/1570180811310040006
DOI https://dx.doi.org/10.2174/1570180811310040006 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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