首页> 中文期刊> 《合成化学》 >N-取代-2-{4,5,6,7-四氢噻吩并3,2-c吡啶-5-基}乙酰胺的合成及其抗血小板聚集活性

N-取代-2-{4,5,6,7-四氢噻吩并3,2-c吡啶-5-基}乙酰胺的合成及其抗血小板聚集活性

         

摘要

Nine novel ADP receptor inhibitors, N-substituted-2-|4,5,6,74,5,6,7-tetrahydrothieno [3,2-c]pyridine-5-yl|acetamides(la~le, 2a~2d), were synthesized from 4,5,6,7-tetrahydrothi-eno[3,2-c]pyridine hydrochloride and 2-oxo-2,4,5,6,7,7a-hexahydrothieno[3,2-c]pyridine hydro-chloride in yields of 61.4% -80.3%. The structures were characterized by 1H NMR and HR-MS. The anti-plated aggregation activities were evaluated by plated aggregation inhibition tests in rats. The results showed that 1 and 2 exhibited certain anti-platelet aggregation activities, in which the inhibitions of 1d and 2d were 50.0% and 58.9% , respectively. The inhibition of 2d was better than the positive control of ticlopidine.%以4,5,6,7-四氢噻吩并[3,2-c]毗啶盐酸盐和2-氧代-2,4,5,6,7,7a-六氢噻吩并[3,2-c]吡啶盐酸盐为起始原料,合成了9个未见文献报道的ADP受体拮抗剂——N-取代-2-14,5,6,7-四氢噻吩并[3,2-c]吡啶-5-基}乙酰胺(1a~1e,2a~2d),收率61.4%-80.3%,其结构经1H NMR和HR-MS表征.大鼠体内抗血小板聚集活性研究表明,1和2均有一定的抗血小板聚集作用,其中1d和2d的作用较强,抑制效率分别为50.0%和58.9%,且2d的抑制作用优于阳性对照药噻氯匹定.

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