Camehn R, Rehse K
Institut für Pharmazie, Freie Universität Berlin, Germany.
Arch Pharm (Weinheim). 2000 May;333(5):130-4. doi: 10.1002/(sici)1521-4184(20005)333:5<130::aid-ardp130>3.0.co;2-d.
Six N-(1-cyanocyclohexyl)-C-phenylnitrones 4a-f (4b-f for the first time) and 22 glyoxaldinitrones 7a-v were prepared and tested for antithrombotic (p.o. administration to rats, 60 mg/kg) effects. Both classes of compounds exhibit considerable antithrombotic activities. Maximum inhibition of thrombus formation in arterioles (21%) was observed in N,N'-bis-2-phenylethylglyoxaldinitrone (7o) and N,N'-bis-4-nitrobenzylglyoxaldinitrone (7u). The compounds form only small amounts of nitric oxide in vitro by the addition of a Fe(3+)-porphyrine complex and an oxygen donor.
制备了六种N-(1-氰基环己基)-C-苯基硝酮4a-f（首次制备了4b-f）和22种乙二醛二硝酮7a-v，并对其抗血栓形成作用（以60mg/kg的剂量口服给予大鼠）进行了测试。这两类化合物均表现出显著的抗血栓活性。在N,N'-双-2-苯乙基乙二醛二硝酮（7o）和N,N'-双-4-硝基苄基乙二醛二硝酮（7u）中观察到对小动脉血栓形成的最大抑制率（21%）。通过添加Fe(3+) -卟啉配合物和氧供体，这些化合物在体外仅形成少量一氧化氮。
