TY - JOUR
T1 - Aza analogs of flavones as potential antimicrobial agents
AU - Sharma, Sahil
AU - Thakur, Vikas
AU - Ojha, Ritu
AU - Budhiraja, Abhishek
AU - Nepali, Kunal
AU - Singh Bedi, Preet Mohinder
PY - 2013/5/1
Y1 - 2013/5/1
N2 - 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 2 nd position of the analogs was also observed.
AB - 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 2 nd position of the analogs was also observed.
KW - Antibacterial
KW - Antifungal
KW - Antimicrobial activity
KW - Flavones
KW - Quinolones
KW - Strains
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U2 - 10.2174/1570180811310040006
DO - 10.2174/1570180811310040006
M3 - Article
AN - SCOPUS:84879765157
SN - 1570-1808
VL - 10
SP - 327
EP - 334
JO - Letters in Drug Design and Discovery
JF - Letters in Drug Design and Discovery
IS - 4
ER -