Ghali N I, Venton D L, Hung S C, Le Breton G C
J Med Chem. 1983 Jul;26(7):1056-60. doi: 10.1021/jm00361a020.
Two new azaprostanoids, a hydrazone (3) and hydrazide (4), have been prepared by the condensation of 2-(6-carboxyhexyl)cyclopentanone with n-hexylhydrazine and caproic acid hydrazide. Preliminary results with the stable hydrazide 4 indicate that it inhibits arachidonic acid (AA) induced human platelet aggregation and that, unlike 13-azaprostanoic acid (1), its site of action is at the cyclooxygenase level. Results with the unstable hydrazone derivative 3 indicate it to be a potent and time-dependent inhibitor of AA-induced human platelet aggregation, with its site of action also at the cyclooxygenase level.
通过2-(6-羧基己基)环戊酮与正己基肼和己酸酰肼缩合制备了两种新的氮杂前列腺素,一种腙(3)和酰肼(4)。稳定的酰肼4的初步结果表明,它能抑制花生四烯酸(AA)诱导的人血小板聚集,并且与13-氮杂前列腺酸(1)不同,其作用位点在环氧化酶水平。不稳定的腙衍生物3的结果表明,它是AA诱导的人血小板聚集的强效和时间依赖性抑制剂,其作用位点也在环氧化酶水平。