Lamotte-Brasseur J, Heymans F, Dive G, Lamouri A, Batt J P, Redeuilh C, Hosford D, Braquet P, Godfroid J J
Centre d'Ingéniérie des Protéines, Institut de Chimie, Liége-Sart-Tilman, Belgium.
Lipids. 1991 Dec;26(12):1167-71. doi: 10.1007/BF02536524.
Nine simple and structurally flexible PAF antagonists were synthesized and their inhibitory effects on PAF induced platelet aggregation were measured. Compounds with PAF antagonistic activity exhibited a negative electrostatic potential generated by two trimethoxyphenyl groups (isocontour at -10 Kcal/mole) at various distances between the negative clouds. The optimal distance between the atoms generating the "cache-oreilles" system for exhibiting potent PAF antagonistic activity is estimated to be 11-13 A. In the flexible molecules studied, the dispersion of the electronic distribution is not necessarily favorable for anti-PAF activity. The data support the simple bipolarized model for the PAF receptor that has been proposed by the authors.
合成了9种简单且结构灵活的血小板活化因子（PAF）拮抗剂，并测定了它们对PAF诱导的血小板聚集的抑制作用。具有PAF拮抗活性的化合物在负电荷云之间的不同距离处表现出由两个三甲氧基苯基产生的负静电势（等势线为-10千卡/摩尔）。产生“窃听器”系统以展现强效PAF拮抗活性的原子之间的最佳距离估计为11 - 13埃。在所研究的柔性分子中，电子分布的分散不一定有利于抗PAF活性。这些数据支持了作者提出的PAF受体的简单双极化模型。
