摘要
为寻找高效抗血小板药物,本文依据某些天然和合成的抗血小板药物的构效关系,设计合成了7-取代异喹啉、8-取代喹啉和烯胺及肟醚的衍生物共16个。初步药理试验表明,大部分化合物对胶原诱导的兔血小板聚集有不同程度的抑制作用。体内试验显示,化合物I_(10),I_4,I_7等对花生四烯酸引起的小白鼠突然死亡有一定的保护作用,其中I_(10)作用最强,在10mg/kg剂量下保护率为72.5%。
Sixteen compounds of 7-substituted isoquinolines, 8-substituted quinolines and some oximinoethers were synthesized and evaluated as platelet aggregation inhibitors. Preliminary pharmacological tests in vitro showed that most of the compounds inhibited collegan-induced rabbit platelet aggregation to a different degree. At dose of 10/kg (ⅳ), compounds Ⅰ_(10), Ⅰ_4 and Ⅰ_7 effectively protected against arachidonic acidinduced sudden death in mice, Ⅰ_(10) was the most active.
出处
《中国药科大学学报》
CAS
CSCD
北大核心
1991年第6期326-329,共4页
Journal of China Pharmaceutical University
关键词
取代异喹啉
喹啉衍生物
合成
活性
7-Substituted isoquinolines
8-Substituted quinolines
Antiplatelet activity
