作者:Klaus Rehse、Tawfig Shahrouri
DOI:10.1002/(sici)1521-4184(199811)331:11<365::aid-ardp365>3.0.co;2-n
日期:1998.11
Twelve ethoxycarbonyl or phenylsulfonyl derivatives as prodrugs of hydroxylamine or phenylhydroxylamine were prepared and tested for antiplatelet (in vitro, Born test) antithrombotic (in vivo thrombosis model), and antihypertensive (in vivo, SHR rats) effects. In the Born test N,N‐bisphenylsulfonylhydroxylamine (10) was most active (IC50 = 11 μmol/L). The N‐ethoxycarbonyl‐phenylhydroxylamine (7) was
制备了 12 种乙氧基羰基或苯磺酰基衍生物作为羟胺或苯羟胺的前药,并测试其抗血小板(体外,Born 试验)抗血栓形成(体内血栓形成模型)和抗高血压(体内,SHR 大鼠)的作用。在 Born 试验 N 中,N-双苯磺酰基羟胺 (10) 的活性最高 (IC50 = 11 μmol/L)。N-乙氧羰基-苯基羟胺 (7) 是最有效的抗血栓化合物。单次口服 60 mg/kg 后,它可抑制大鼠肠系膜小动脉血栓形成 39%。化合物 7 没有任何抗高血压活性。因此,已经有可能将合适的羟胺衍生物的抗血栓形成活性与抗高血压特性完全分开。