Keloth, Kothari Srinivasan and Vachala , Seekarajapuram Dinakaran (2011) Anti-Inflammatory and antimicrobial Potential of some novel fused benzopyrimidine derivatives. Pharmacologyonline, 2. pp. 14-23.

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Abstract

In the present study, a series of novel 2-phenyl-3, 6, 7-trisubstituted quinazolin-4(3H)-ones (ABM 1-8) were synthesized by microwave irradiation method using 2-benzamido benzoic acid and different primary amines. The structure of these compounds was confirmed by IR, 1H-NMR and mass spectral analysis. All the synthesized compounds were tested for their anti-inflammatory activity; in vitro antimicrobial and time kill studies. The anti-inflammatory activity was performed at two different concentrations (50 and 100mg/kg body mass) by rat paw oedema model. Ibuprofen (100mg/kg) was used as standard. Compounds ABM-5 and ABM-7 showed a very good anti-inflammatory activity at 50 and 100mg/kg body weight respectively. Among the ABM series, compound ABM-4 showed microbial growth inhibition at very low concentrations. The minimum inhibitory concentration of ABM-4 against P. aeroginosa, S. aureus, E. coli, C. albicans and A. flavus was found to be 0.78, 0.39, 0.39, 1.56 and 6.25 μg/ml respectively. The most potent compound ABM-4 was then considered for time kill study for 0-24h. It showed 100% growth inhibition at the 12th h against P. aeroginosa. These data revealed that the compounds containing 4-chlorophenyl, N,Ndimethyl ethyl groups and 4-fluorophenyl substitutions at 3rd position in the quinazolinone nucleus played an important role in anti-inflammatory and antimicrobial activities.

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