Urgun H, Balkan A, Ozalp M
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hacettepe University, Ankara, Turkey.
Arzneimittelforschung. 2000 Dec;50(12):1115-9. doi: 10.1055/s-0031-1300338.
In this study, by starting from ethyl 4-amino-2,3-dihydro-3-phenyl-2-thioxothiazole-5-carboxylate (1), three compounds having 2,3-dihydro-3-phenyl-5-mercapto-6-alkyl/phenyl-2-thioxothiazolo[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 microdilution 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.
在本研究中,从4-氨基-2,3-二氢-3-苯基-2-硫代噻唑-5-羧酸乙酯(1)开始,合成了三种具有2,3-二氢-3-苯基-5-巯基-6-烷基/苯基-2-硫代噻唑并[4,5-d]嘧啶-7(6H)-酮(2a - c)结构的化合物及其5-(4'-未取代/-取代苯甲酰甲基)硫代衍生物(3a - l)。采用微量稀释法研究了合成化合物对一些细菌和真菌的抗菌活性。发现对革兰氏阳性菌和类酵母真菌具有显著活性的2,3-二氢-3,6-二苯基-5-(4'-溴苯甲酰甲基)硫代-2-硫代噻唑并[4,5-d]嘧啶-7(6H)酮(3k)是该系列中活性最高的化合物。