Ishikawa F, Saegusa J, Inamura K, Sakuma K, Ashida S
J Med Chem. 1985 Oct;28(10):1387-93. doi: 10.1021/jm00148a003.
A series of novel 1,2,3,5-tetrahydroimidazo[2,1-b]quinazolin-2-one derivatives substituted with a secondary amino group has been prepared and tested for the activities of inhibiting platelet aggregation in rats in vitro and ex vivo. Most of the compounds were found to be the potent inhibitors of platelet aggregation. Some of the active compounds were soluble in water and effective via iv infusion in rats. Structure-activity relationships have indicated that a lipophilic secondary amino group located at position 6 or 7 contributed to retention of potent activity. Among the compounds studied, 7-piperidino-1,2,3,5-tetrahydroimidazo[2,1-b]quinazolin-2- one (13 g,DN-9693) was the most favorable compound.
一系列带有仲氨基取代基的新型1,2,3,5-四氢咪唑并[2,1-b]喹唑啉-2-酮衍生物已被制备，并在大鼠体内外进行了抑制血小板聚集活性的测试。发现大多数化合物是血小板聚集的有效抑制剂。一些活性化合物可溶于水，并且通过静脉输注在大鼠体内有效。构效关系表明，位于6位或7位的亲脂性仲氨基有助于保持强效活性。在所研究的化合物中，7-哌啶基-1,2,3,5-四氢咪唑并[2,1-b]喹唑啉-2-酮（13 g，DN-9693）是最有利的化合物。
