CONDENSATION OF 2-(2-GUANIDINO-4-OXO-4, 5- DIHYDROTHIAZOL-5-YL) ACETIC ACID WITH DICARBONYL COMPOUNDS

A hybrid pharmacophore approach was adopted to design and synthesize new series of pyrimidine-thiazole hybrid compounds via heterocyclization of 2-(2-guanidino-4-oxo-4,5-dihydrothiazol-5-yl)acetic acid with dicarbonyl compounds, such as diketones and derivatives of acetoacetic ester. The structures of the compounds were established by IR, 1H NMR, 13C NMR. The products were obtained in a good yield, short time and a simple experimental procedure. The synthesized compounds were evaluated for their anti-bacterial activity against Grampositive and Gram-negative bacteria. The compounds exhibited excellent zone of inhibition against tested bacteria. The investigation of antifungal screening data revealed that all the tested compounds showed moderate to good fungal inhibition. Keywords: 2-Guanidino-4-thiazolinone-5-yl acetic acid; heterocyclization; Pyrimidine-Thiazole Hybrids, Synthesis, Antimicrobial activity.