Rehse K, Lüdtke E
Institut für Pharmazie, Freien Universität Berlin.
Arch Pharm (Weinheim). 1995 Jan;328(1):17-20. doi: 10.1002/ardp.19953280105.
Twenty 1,3,4-thiadiazole-2-nitrosimines and two 1,2,4-thiadiazole-5-nitrosimines were synthesized and assayed in the Born-test for their antiplatelet activity. Only two 1,3,4-thiadiazoles inhibited the aggregation at IC50 < 10 mumol/L. In an in vivo thrombosis model only in arterioles a small inhibition of thrombus formation was observed. The poor test results correspond to a very high chemical stability of the titel nitrosimines.
合成了20种1,3,4-噻二唑-2-亚硝基胺和2种1,2,4-噻二唑-5-亚硝基胺，并在玻恩试验中测定了它们的抗血小板活性。只有2种1,3,4-噻二唑在IC50 < 10 μmol/L时抑制聚集。在体内血栓形成模型中，仅在小动脉中观察到对血栓形成的轻微抑制。较差的测试结果与标题亚硝基胺非常高的化学稳定性相对应。
