Thromboxane modulating agents .2. Thromboxane receptor antagonists derived from the thromboxane synthase inhibitor dazmegrel

被引：9

作者：

Dickinson, RP

Dack, KN

Steele, J

Tute, MS

机构：

[1] Department of Discovery Chemistry, Pfizer Central Research, Sandwich

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 14期

关键词：

D O I：

10.1016/0960-894X(96)00299-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The design of dual thromboxane synthase inhibitor/thromboxane receptor antagonists (e.g, 15) based on the structure of the thromboxane synthase inhibitor dazmegrel is described. More potent receptor antagonists (e.g, 16c) result from replacement of the pyridinyl subsituent with 4-fluorophenyl. Modelling suggests the existence of more than one site capable of interacting with the aryl sulfonamide of TxA(2) receptor antagonists. Copyright (C) 1996 Elsevier Science Ltd

引用

页码：1691 / 1696

页数：6

共 23 条

[1]

Bhagwat Shripad S., 1994, Drugs of the Future, V19, P765

[2]

COLLINGTON EW, 1990, ANNU REP MED CHEM, V25, P99

[3]

COOPER DG, 1990, Patent No. 365183

[4] IDENTIFICATION OF A CRUCIAL SUBSTRUCTURAL UNIT FOR THROMBOXANE-A2 RECEPTOR-BINDING [J].