Biftu T, Gamble N F, Doebber T, Hwang S B, Shen T Y, Snyder J, Springer J P, Stevenson R
J Med Chem. 1986 Oct;29(10):1917-21. doi: 10.1021/jm00160a020.
The six (racemic or meso) isomers of 3,4-dimethyl-2,5-bis(3,4-dimethoxyphenyl)tetrahydrofuran and four corresponding desmethyl analogues were prepared and assayed as inhibitors of platelet activating factor (PAF) receptor binding to rabbit platelet plasma membranes. The inhibition by these isomers is stereodependent and varies with the gross shape of the molecules as determined by the molecular mechanics program MM2. The most potent PAF antagonist in this group of compounds is trans-2,5-bis(3,4,5-trimethoxyphenyl)tetrahydrofuran (L-652,731, 14) with an IC50 of 0.02 microM.
制备了3,4-二甲基-2,5-双（3,4-二甲氧基苯基）四氢呋喃的六种（外消旋或内消旋）异构体和四种相应的去甲基类似物，并作为血小板活化因子（PAF）受体与兔血小板质膜结合的抑制剂进行了测定。这些异构体的抑制作用具有立体依赖性，并且根据分子力学程序MM2确定的分子总体形状而有所不同。该组化合物中最有效的PAF拮抗剂是反式-2,5-双（3,4,5-三甲氧基苯基）四氢呋喃（L-652,731, 14），IC50为0.02微摩尔。
