Rehse K, Brümmer U, Unsöld E
Institut für Pharmazie, Freie Universität Berlin, Germany.
Pharmazie. 1998 Dec;53(12):820-4.
The successful synthesis of 17 nitrosimines of 2 H-1,3,4-thiadiazines is reported. They are best characterized by their electronic spectra (lambda max = 504-522 nm). Some of the compounds were able to inhibit the aggregation of blood platelets in the Born-test (inducer collagen). The most active compound was the 3-nonyl-5-phenyl-derivative 10c which showed an IC50 = 6.5 mumol.l-1. In mesenteric arterioles of rats after p.o. administration (60 mg/kg) a 13% inhibition of thrombus formation is observed. The reason for the rather small effects is the high chemical stability of the title compounds and the fact that decomposition occurs mainly by the evolution of molecular nitrogen. Only small yields of NO are formed.
报道了2H-1,3,4-噻二嗪的17种亚硝基胺的成功合成。它们的最佳表征是通过其电子光谱（λmax = 504 - 522 nm）。一些化合物能够在博恩试验（诱导剂胶原蛋白）中抑制血小板聚集。活性最高的化合物是3-壬基-5-苯基衍生物10c，其IC50 = 6.5 μmol·L-1。在大鼠口服给药（60 mg/kg）后，在肠系膜小动脉中观察到血栓形成受到13%的抑制。效果相对较小的原因是标题化合物的高化学稳定性以及分解主要通过分子氮的释放发生这一事实。仅形成少量的一氧化氮。
