Synthesis and anti-microbial screening of some new 6,7,8,9-Tetrahydro-5H-5-(2'-hydroxyphenyl)-2-(4'- substitutedbenzylidine)-3-(4-nitrophenylamino) thiazoloquinazoline derivatives

Order of Publishing in Issue: 
9
Volume :4
Issue :2
April, 2010 - June, 2010
Page No: 
708-715
Authors: 
Theivendren Panneer Selvam [1]* and Palanirajan Vijayaraj Kumar [2]
Address: 
[1] D.C.R.M. Pharmacy College, Inkollu- 523 167, Andhra Pradesh, India.
Address: 
[2] Bharat Institute of Technology (Pharmacy), Hyderabad-501 510, Andhrapredesh, India.
Email-ID: 
tpsphc@gmail.com

Abstract : A series of some new 6,7,8,9-Tetrahydro-5H-5- (2'-hydroxyphenyl)-2-(4'-fluorobenzylidine)-3-(4- nitrophenyl amino) thiazolo quinazoline (4a-4d) and 6,7,8,9-Tetrahydro-5H-5-(2'-hydroxy phenyl)- 2-(4'-substituted benzylidine)-3-(4-nitrophenylamino) thiazolo quinazoline (5a-5d) derivatives were synthesized. The in vitro anti-bacterial and anti-fungal activities were determined by paperdisk diffusion method. The minimum inhibitory concentrations (MIC) of the compounds were also determined by agar streak dilution method.Most of the synthesized compounds exhibited significant anti-bacterial and anti-fungal activities. Among the synthesized compounds 6,7,8,9-Tetrahydro-5H-5-(2'-hydroxy phenyl)-2-(4'-methoxy benzylidine)-3-(4-nitro phenyl amino)thiazolo quinazoline 5a, 6,7,8,9-Tetrahydro-5H-5-(2'-hydroxyphenyl)-2-(3',4'-dimethyl benzylidine)-3-(4- nitrophenyl amino) thiazolo quinazoline 5b and 6,7,8,9-Tetrahydro-5H-5-(2'-hydroxyphenyl)-2-(4'-fluoro benzylidine)-3-(4-nitro phenylamino) thiazolo quinazoline 5d exhibited most potent in vitro antimicrobial activity with MIC of (9.4, 10.2,10.4, 10.2, 11.3, 12.1, 12.7, 14.6, 18.7), (10.3, 14.2, 11.6, 13.4, 13.6, 13.8, 14.6, 13.1, 14.5) and (12.5, 10.3, 14.1, 10.6, 13.4, 19.8, 17.8, 11.2, 13.6) at 100 ?g mL-1 against Staphylococcus aureus, Staphylococcusepidermidis, Micrococcus luteus, Bacillus cereus, Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae,Aspergillus niger and Candida albicans.
 

Keywords: 
Thiazoloquinazoline, Benzylidine thiazoloquinazoline, Nitrophenyl amino Thiazoloquinazoline, Dimethyl group substitution, anti-bacterial, anti-fungal.
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