ONE-POT THREE-COMPONENT MICROWAVE-ASSISTED SYNTHESIS OF NOVEL THIAZOLIDINONE DERIVATIVES CONTAINING THIENO[d]PYRIMIDINE-4-ONE MOIETY AS POTENTIAL ANTIMICROBIAL AGENTS

2015 I. H. El Azab*, **, # and Sh. H. Abdel-Hafez*, ***

#Phone: +2097480446; fax: +2097480450; e-mail: ihelmy2003@yahoo.com; i.helmy@tu.edu.sa

*Chemistry Department, Faculty of Science, Taif University, Al-Haweiah, Taif, 21974 Saudi Arabia;
**Chemistry Department, Faculty of Science, Aswan University, Aswan, 81528 Egypt;
***Chemistry Department, Faculty of Applied Science, Assiut University, Assiut, Egypt

New 2-methyl-5-(4-oxo-2-(substituted phenyl)thiazolidin-3-yl)thieno[3,4-d]-pyrimidin-4-one, 5-(2,7-diphenyl-5-thioxo-5,6,7,7a-tetrahydrothiazolo[4,5-d]pyrimidin-3(2H)-yl)-2-methylthieno[3,4-d]pyrimidin-4(3H)-one, and 2-methyl-5-(5-phenyl-thiazolo[5,4-d]isoxazol-6(5H)-yl)thieno[3,4-d]pyrimidin-4(3H)-one have been prepared under microwave-assisted and conventional conditions. The new compounds were screened for their in vitro antimicrobial activity against two gram-positive bacteria (Bacillus subtilis NCIM-2063 and Staphylococcus aureus NCIM-2901), one gram-negative bacteria (Escherichia coli NCIM-2256), and three fungal strains (Candida albicans NCIM-3471, Aspergillus flavus NCIM-539, and Aspergillus niger NCIM-1196) and showed promising biological activity.

Keywords: 4-thiazolidinone derivatives, microwave-assisted synthesis, antimicrobial activity, cytotoxicity.