THROMBOXANE RECEPTOR ANTAGONISM COMBINED WITH THROMBOXANE SYNTHASE INHIBITION .7. PYRIDINYLALKYL-SUBSTITUTED ARYLSULFONYLAMINO ARYLALKANOIC ACIDS

被引：12

作者：

BHAGWAT, SS

ROLAND, DM

MAIN, AJ

GUDE, C

GRIM, K

GOLDSTEIN, R

COHEN, DS

DOTSON, R

MATHIS, J

LEE, W

机构：

[1] Research Department, Pharmaceuticals Division, CIBA-GEIGY Corporation, Summit, NJ 07901

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1992年 / 2卷 / 12期

关键词：

D O I：

10.1016/S0960-894X(00)80443-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Arylsulfonylamino arylalkanoic acids substituted with a pyridinylalkyl group on the arylalkanoic acid portion of the molecule were synthesized and found to behave as thromboxane receptor antagonists (TxRAs) and thromboxane synthase inhibitors (TxSls). One of these compounds (11), with a 1,3,5-trisubstituted central aromatic ring was demonstrated lo have good functional bioavailability and efficacy as a platelet inhibitor in guinea pigs.

引用

页码：1623 / 1626

页数：4

共 8 条

[1]

AMES DE, 1981, SYNTHESIS-STUTTGART, P364

[2] THROMBOXANE RECEPTOR ANTAGONISM COMBINED WITH THROMBOXANE SYNTHASE INHIBITION .1. (+/-)-(3-PYRIDINYLBICYCLOHEPTYL)ALKANOIC ACIDS [J].