Demchenko Anatoly, Bobkova Ludmila, Yadlovskiy Oleh, Buchtiarova Tatiana, Demchenko Sergey
Institute of Pharmacology and Toxicology, Eugene Pottier 14, 03057 Kiev, Ukraine.
Sci Pharm. 2016 Apr-Jun;84(2):255-68. doi: 10.3797/scipharm.1505-16. Epub 2015 Aug 27.
A series of novel 2-(N-pyrrolidino, N-piperidino or N-morpholino)-7-phenyl(α-furoyl or α-thienyl)-[1,3]thiazolo[4,5-d]pyridazinones 10a-c, 14-16a,b was synthesized in 78-87% yields via the reaction of methyl 5-benzoyl(α-furoyl or α-thienyl)-2-aminosubstituted-thiazol-4-carboxylates 9a-c, 13a-e with hydrazine. These new compounds have been tested for their in vivo analgesic and anti-inflammatory activities. All compounds have been characterized by (1)H-NMR, (13)C-NMR spectroscopy, and liquid chromatography-mass spectrometry.
通过5-苯甲酰基(α-呋喃甲酰基或α-噻吩甲酰基)-2-氨基取代的噻唑-4-羧酸甲酯9a-c、13a-e与肼反应,以78-87%的产率合成了一系列新型的2-(N-吡咯烷基、N-哌啶基或N-吗啉基)-7-苯基(α-呋喃甲酰基或α-噻吩甲酰基)-[1,3]噻唑并[4,5-d]哒嗪酮10a-c、14-16a、b。已对这些新化合物的体内镇痛和抗炎活性进行了测试。所有化合物均通过(1)H-NMR、(13)C-NMR光谱和液相色谱-质谱进行了表征。