ICI 180080，一种新型选择性血栓素受体拮抗剂：合成及相对活性

ICI 180080, a novel selective thromboxane receptor antagonist: synthesis and relative activity.

作者信息

Brown G R, Foubister A J

出版信息

J Pharm Pharmacol. 1986 Sep;38(9):706-8. doi: 10.1111/j.2042-7158.1986.tb03117.x.

DOI:10.1111/j.2042-7158.1986.tb03117.x

Abstract

The preparation of a novel potent thromboxane receptor antagonist ICI 180080, 5(Z)-7-[2,2-dimethyl-4-(2-hydroxyphenyl)-1,3-dioxan-cis-5-yl] heptenoic acid, is described together with its methyl ether and methyl ester. Thromboxane antagonist pA2 data against U 46619 is presented for rabbit thoracic aorta in-vitro (ICI 180080, pA2 = 7.5). The relative antagonist pA2 values obtained are discussed in terms of the chemical structure of the molecules. The potent activity of ICI 180080 is attributed to a specific orientation of the phenolic oxygen, due to an intramolecular hydrogen bond.

摘要

本文描述了一种新型强效血栓素受体拮抗剂ICI 180080，即5(Z)-7-[2,2-二甲基-4-(2-羟基苯基)-1,3-二氧杂环己烷-顺-5-基]庚烯酸及其甲酯和甲醚。给出了兔胸主动脉体外针对U 46619的血栓素拮抗剂pA2数据（ICI 180080，pA2 = 7.5）。根据分子的化学结构对获得的相对拮抗剂pA2值进行了讨论。ICI 180080的强效活性归因于酚氧由于分子内氢键而具有的特定取向。