Nonpeptide GPIIb/IIIa inhibitors .10. Centrally constrained alpha-sulfonamides are potent inhibitors of platelet aggregation

被引：45

作者：

Egbertson, MS ^{[1
]}

Hartman, GD ^{[1
]}

Gould, RJ ^{[1
]}

Bednar, B ^{[1
]}

Bednar, RA ^{[1
]}

Cook, JJ ^{[1
]}

Gaul, SL ^{[1
]}

Holahan, MA ^{[1
]}

Libby, LA ^{[1
]}

Lynch, JJ ^{[1
]}

Lynch, RJ ^{[1
]}

Sitko, GR ^{[1
]}

Stranieri, MT ^{[1
]}

Vassallo, LM ^{[1
]}

机构：

[1] MERCK RES LABS,DEPT PHARMACOL,W POINT,PA 19486

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 21期

关键词：

D O I：

10.1016/0960-894X(96)00473-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Potency enhancing features of two series of fibrinogen receptor antagonists were combined to give analogs with improved potency and oral activity. Antagonists containing either alkyl or aryl sulfonamides and a central isoindolinone structural constraint demonstrate high affinity for both activated and unactivated platelet receptors. Copyright (C) 1996 Elsevier Science Ltd

引用

页码：2519 / 2524

页数：6

共 10 条

[1]

Cook Nigel S., 1994, Drugs of the Future, V19, P135

[2] Non-peptide glycoprotein IIb/IIIa inhibitors .9. Centrally constrained alpha-sulfonamides are useful tools for exploring platelet receptor function [J].

Egbertson, MS ;

Bednar, B ;

Bednar, RA ;

Hartman, GD ;

Gould, RJ ;

Lynch, RJ ;

Vassallo, LM ;

Young, SD .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1996, 6 (12) :1415-1420

[3] A SELECTIVE PROTECTION OF 2,3-DIAMINOPROPIONIC ACID [J].

EGBERTSON, MS ;

HOMNICK, CF ;

HARTMAN, GD .

SYNTHETIC COMMUNICATIONS, 1993, 23 (05) :703-709

[4] NONPEPTIDE FIBRINOGEN RECEPTOR ANTAGONISTS .2. OPTIMIZATION OF A TYROSINE TEMPLATE AS A MIMIC FOR ARG-GLY-ASP [J].

EGBERTSON, MS ;

CHANG, CTC ;

DUGGAN, ME ;

GOULD, RJ ;

HALCZENKO, W ;

HARTMAN, GD ;

LASWELL, WL ;

LYNCH, JJ ;

LYNCH, RJ ;

MANNO, PD ;

NAYLOR, AM ;

PRUGH, JD ;

RAMJIT, DR ;

SITKO, GR ;

SMITH, RS ;

TURCHI, LM ;

ZHANG, GX .

JOURNAL OF MEDICINAL CHEMISTRY, 1994, 37 (16) :2537-2551

[5] NONPEPTIDE FIBRINOGEN RECEPTOR ANTAGONISTS .3. DESIGN AND DISCOVERY OF A CENTRALLY CONSTRAINED INHIBITOR [J].

EGBERTSON, MS ;

NAYLOR, AM ;

HARTMAN, GD ;

COOK, JJ ;

GOULD, RJ ;

HOLAHAN, MA ;

LYNCH, JJ ;

LYNCH, RJ ;

STRANIERI, MT ;

VASSALLO, LM .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1994, 4 (15) :1835-1840

[6] NONPEPTIDE FIBRINOGEN RECEPTOR ANTAGONISTS .1. DISCOVERY AND DESIGN OF EXOSITE INHIBITORS [J].

HARTMAN, GD ;

EGBERTSON, MS ;

HALCZENKO, W ;

LASWELL, WL ;

DUGGAN, ME ;

SMITH, RL ;

NAYLOR, AM ;

MANNO, PD ;

LYNCH, RJ ;

ZHANG, GX ;

CHANG, CTC ;

GOULD, RJ .

JOURNAL OF MEDICINAL CHEMISTRY, 1992, 35 (24) :4640-4642

[7]

KOUNS WC, 1992, J BIOL CHEM, V267, P18844

[8]

LYNCH JJ, 1995, J PHARMACOL EXP THER, V272, P20

[9]

PHILIPS DR, 1990, ANN REV CELL BIOL, V6, P329

[10]

PHILLIPS DR, 1988, BLOOD, V71, P831

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