Nonpeptide glycoprotein IIb/IIIa inhibitors: Substituted quinazolinediones and quinazolinones as potent fibrinogen receptor antagonists

被引:128
作者
Liverton, NJ
Armstrong, DJ
Claremon, DA
Remy, DC
Baldwin, JJ
机构
[1] Merck Sharp & Dohme Ltd, Res Labs, Dept Med Chem, W Point, PA 19486 USA
[2] Merck Sharp & Dohme Ltd, Res Labs, Dept Pharmacol, W Point, PA 19486 USA
关键词
D O I
10.1016/S0960-894X(98)00047-X
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis and biological activity of a series of 3,6-substituted quinazolinediones and quinazolinones are described. The potent activity of these compounds as platelet aggregation inhibitors demonstrates the utility of these structures as central templates for nonpeptide RGD mimics. (C) 1998 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:483 / 486
页数:4
相关论文
共 15 条
[1]   PALLADIUM-CATALYZED FORMYLATION OF ORGANIC HALIDES WITH CARBON-MONOXIDE AND TIN HYDRIDE [J].
BAILLARGEON, VP ;
STILLE, JK .
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1986, 108 (03) :452-461
[2]   PLATELETS AND THROMBOLYTIC THERAPY [J].
COLLER, BS .
NEW ENGLAND JOURNAL OF MEDICINE, 1990, 322 (01) :33-42
[3]  
Cook Nigel S., 1994, Drugs of the Future, V19, P135
[4]   SELECTIVE OXIDATION OF ALDEHYDES TO CARBOXYLIC-ACIDS WITH SODIUM-CHLORITE HYDROGEN-PEROXIDE [J].
DALCANALE, E ;
MONTANARI, F .
JOURNAL OF ORGANIC CHEMISTRY, 1986, 51 (04) :567-569
[5]   Nonpeptide GPIIb/IIIa inhibitors .10. Centrally constrained alpha-sulfonamides are potent inhibitors of platelet aggregation [J].
Egbertson, MS ;
Hartman, GD ;
Gould, RJ ;
Bednar, B ;
Bednar, RA ;
Cook, JJ ;
Gaul, SL ;
Holahan, MA ;
Libby, LA ;
Lynch, JJ ;
Lynch, RJ ;
Sitko, GR ;
Stranieri, MT ;
Vassallo, LM .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1996, 6 (21) :2519-2524
[6]   A SELECTIVE PROTECTION OF 2,3-DIAMINOPROPIONIC ACID [J].
EGBERTSON, MS ;
HOMNICK, CF ;
HARTMAN, GD .
SYNTHETIC COMMUNICATIONS, 1993, 23 (05) :703-709
[7]   NEW PALLADIUM MEDIATED CYCLOPENTANATION OF ALKENES BEARING A DELTA NUCLEOPHILIC SUBSTITUENT [J].
FOURNET, G ;
BALME, G ;
GORE, J .
TETRAHEDRON LETTERS, 1989, 30 (01) :69-70
[8]  
GAN ZR, 1988, J BIOL CHEM, V263, P19827
[9]   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
[10]  
KNOEBEL SB, 1989, J AM COLL CARDIOL, V14, P813