A pharmacophore model for sulphonyl-urea (-cyanoguanidine) compounds with dual action, thromboxane receptor antagonists and thromboxane synthase inhibitors

被引：9

作者：

Michaux, C

Dogné, JM

Rolin, S

Masereel, B

Wouters, J

Durant, F

机构：

[1] Fac Univ Notre Dame Paix, Lab Chim Mol Struct, B-5000 Namur, Belgium

[2] Univ Liege, Ulg, Ctr Interfac Rech Pharmacochim Subst Nat & Synth, Lab Chim Pharmaceut, B-4000 Liege, Belgium

[3] Fac Univ Notre Dame Paix, Dept Pharm, B-5000 Namur, Belgium

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2003年 / 38卷 / 7-8期

关键词：

pharmacophore; thromboxane receptor antagonism; thromboxane synthase inhibition; sulphonyl-urea (-cyanoguanidine) ligand; catalyst hypothesis;

D O I：

10.1016/S0223-5234(03)00076-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A 3D pharmacophore model was developed for original sulphonyl-urea (-cyanoguanidine) compounds and known molecules which behave both as thromboxane receptor antagonists and as thromboxane synthase inhibitors. Five recognition sites appear to be essential for this dual activity: two hydrogen bond acceptors, an anionic site, a hydrophobic group and an aromatic ring. Such a model could be used to design new leads possessing the same pharmacological profile and to improve the activity of our compounds. (C) 2003 Editions scientifiques et medicales Elsevier SAS. All rights reserved.

引用

页码：703 / 710

页数：8

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