Tanaka A, Murata M, Fujiwara H
Basic Research Laboratories, Fujisawa Pharmaceutical Co. Ltd., Osaka, Japan.
Bioorg Med Chem Lett. 1998 Sep 22;8(18):2483-8. doi: 10.1016/s0960-894x(98)00405-3.
A QSAR study using the novel hydrophobic descriptor (logPmw), which is a descriptor for membrane affinity, of our fibrinogen inhibitors FK633 (1), FR158999 (21), and related derivatives was performed, and resulted in good correlation (n = 19, s = 0.268, F = 6.38**, r = 0.667). Based on these results, we constructed a hypothesis by which these potent inhibitors bind to the receptor via the biomembrane and the C-terminal moiety functions as an anchor moiety.
使用新型疏水描述符（logPmw）对我们的纤维蛋白原抑制剂FK633（1）、FR158999（21）及相关衍生物进行了定量构效关系（QSAR）研究，该描述符是一种膜亲和力描述符，研究得到了良好的相关性（n = 19，s = 0.268，F = 6.38**，r = 0.667）。基于这些结果，我们构建了一个假设，即这些强效抑制剂通过生物膜与受体结合，且C末端部分起锚定部分的作用。
