New Thiazolo[4,5-d]pyrimidine Derivatives as Potential Antimicrobial Agents

Summary

In this study, by starting from ethyl 4-amimo-2,3-dihydro-3-phenyl-2-thioxothiazole-5-carboxylate (1), three compounds having 2,3-dihydro-3-phenyl-5-mercapto-6-alkyl/phenyl-2-thi-oxothiazolo[4,5-d]pyrimidin-7(6H)-one (2a-c) structure and their 5-(4’-nonsubstituted/-substituted benzoylmethyl)thio derivatives (3a-l) were synthesized. The antimicrobial activities of the synthesized compounds were investigated against some bacteria and fungi using the micro-dilution method. 2.3- Dihydro- 3,6-diphenyl- 5- (4’-bromobenzoylmethyl) thio- 2-thioxothiazolo [4,5-d]pyrimidin-7(6H) one (3k) possessing remarkable activity against Gram-positive bacteria and yeast like fungi was found to be the most active compound in this series.

Zusammenfassung

Neue Thiazolo [4,5-d]pyrimidin-Derivate als potentielle antimikrobielle Wirkstoffe In dieser Arbeit wurden drei 2,3-Dihydro-3-phenyl-5-mercapto-6-alkyl/phenyl-2-thioxothia-zolo[4,5-d]pyrimidin-7(6H)-one (2a-c) und ihre neuen 5-(4’-Nonsubstitutierte/-substitutierte Benzoylmethyl) thio-Derivative (3a-l) hergestellt. Ihre antimikrobielle Wirkung in vitro gegen Gram-positive Bakterien und Candida-Hefen mit Hilfe von Reihenverdünnungstests untersucht. Substanz 3k, 2,3-Dihydro-3,6-diphenyl-5-(4’-bromobenzoylmethyl)thio-2-thioxothia-zolo[4,5-d]pyrimidin-7(6H)-on, zeigte gegen Gram-positive Bakterien und Candida-Hefen die beste Wirkung.

Key words

2-Thioxothiazolo[4,5-d]pyrimidin-7(6H)-ones, antibacterial activity - antifungal activity, in vitro studies, synthesis