Rehse K, Schleifer K J
Institut für Pharmazie der Freien Universität Berlin.
Arch Pharm (Weinheim). 1993 Dec;326(12):929-39. doi: 10.1002/ardp.19933261204.
38 title compounds have been synthesized. They bear a wide variety in substituents including alkyl-, aryl-, arylalkyl-, and styryl groups. The anti-platelet activities elucidated in the Born-test with collagen cover more than two orders of magnitude (IC50 = 0.3-45 mumol/L). These effects depend on the presence of the N-NO-group. This is shown by comparison with the corresponding sydnone imines, sydnone cyanimines, and sydnones. The most suitable substituents were phenylethyl, styryl, and hexyl at either position of the molecule. Seven compounds, most of them styryl derivatives, have IC50 values below 1 mumol/L. It is suggested that the differences in activity are connected with the ability of the compounds to bind to the platelet membrane.
已合成了38种标题化合物。它们带有各种各样的取代基，包括烷基、芳基、芳烷基和苯乙烯基。在与胶原蛋白的博恩试验中阐明的抗血小板活性涵盖了两个多数量级（IC50 = 0.3 - 45 μmol/L）。这些效应取决于N - NO基团的存在。通过与相应的斯德酮亚胺、斯德酮氰胺和斯德酮进行比较得以证明。分子任一位置上最合适的取代基是苯乙基、苯乙烯基和己基。七种化合物，其中大多数是苯乙烯基衍生物，其IC50值低于1 μmol/L。有人认为活性差异与化合物结合血小板膜的能力有关。
