SYNTHESIS OF PYRROLIDINE OXAZOLES AS THROMBOXANE-A(2) ENDOPEROXIDE RECEPTOR ANTAGONISTS

被引：3

作者：

HALL, SE

HAN, WC

HARRIS, DN

GOLDENBERG, H

MICHEL, IM

MONSHIZADEGAN, H

WEBB, ML

机构：

[1] Bristol-Myers Squibb, Pharmaceutical Research Institute, Princeton, NJ 08543-4000

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1993年 / 3卷 / 06期

关键词：

D O I：

10.1016/S0960-894X(00)80328-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis and antiplatelet activity of a series of bis-heterocyclic thromboxane A2 receptor antagonists is described. The L-proline analog 9 was the most potent ligand in this class with a K(D) = 7.9+/-0.71 nM in washed human platelets.

引用

页码：1263 / 1266

页数：4

共 11 条

[1] THROMBOXANE A2 RECEPTOR ANTAGONISTS [J].

HALL, SE .

MEDICINAL RESEARCH REVIEWS, 1991, 11 (05) :503-579

[2]

HALUSHKA P V, 1989, Drugs of Today, V25, P383

[3] THROMBOXANES - NEW GROUP OF BIOLOGICALLY-ACTIVE COMPOUNDS DERIVED FROM PROSTAGLANDIN ENDOPEROXIDES [J].

HAMBERG, M ;

SVENSSON, J ;

SAMUELSSON, B .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1975, 72 (08) :2994-2998

[4] 9-ALPHA-HOMO-9,11-EPOXY-5,13-PROSTADIENOIC ACID ANALOGS - SPECIFIC STABLE AGONIST (SQ 26,538) AND ANTAGONIST (SQ 26,536) OF THE HUMAN-PLATELET THROMBOXANE RECEPTOR [J].

HARRIS, DN ;

PHILLIPS, MB ;

MICHEL, IM ;

GOLDENBERG, HJ ;

HEIKES, JE ;

SPRAGUE, PW ;

ANTONACCIO, MJ .

PROSTAGLANDINS, 1981, 22 (02) :295-307

[5]

HEDBERG A, 1988, J PHARMACOL EXP THER, V245, P786

[6]

LEFER A M, 1988, Drugs of the Future, V13, P999

[7] THROMBOXANE RECEPTOR ANTAGONIST BMS-180291 - A NEW PRECLINICAL LEAD [J].

MISRA, RN ;

BROWN, BR ;

SHER, PM ;

PATEL, MM ;

HALL, SE ;

HAN, WC ;

BARRISH, JC ;

FLOYD, DM ;

SPRAGUE, PW ;

MORRISON, RA ;

RIDGEWELL, RE ;

WHITE, RE ;

DIDONATO, GC ;

HARRIS, DN ;

HEDBERG, A ;

SCHUMACHER, WA ;

WEBB, ML ;

OGLETREE, ML .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1992, 2 (01) :73-76

[8] INTERPHENYLENE 7-OXABICYCLO[2.2.1]HEPTANES - SQ-33961 - A NEW POTENT, LONG-ACTING THROMBOXANE ANTAGONIST [J].

MISRA, RN ;

BROWN, BR ;

SHER, PM ;

PATEL, MM ;

GOLDENBERG, HJ ;

MICHEL, IM ;

HARRIS, DN .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1991, 1 (09) :461-464

[9]

OGLETREE ML, 1987, FED PROC, V46, P133

[10]

OGLETREE ML, 1991, CIRCULATION, V84, P79

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