Design and synthesis of a novel class of thrombin inhibitors incorporating heterocyclic dipeptide surrogates

被引:38
|
作者
Tamura, SY
Semple, JE
Reiner, JE
Goldman, EA
Brunck, TK
LimWilby, MS
Carpenter, SH
Rote, WE
Oldeshulte, GL
Richard, BM
Nutt, RF
Ripka, WC
机构
[1] Department of Medicinal Chemistry, Corvas International, Inc., San Diego, CA 92121
关键词
D O I
10.1016/S0960-894X(97)00258-8
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Several potent and selective inhibitors of thrombin incorporating novel heterocyclic peptide surrogates in the P-3-P-2 position of peptidyl argininals have been discovered. Illustrated in this article are three classes of heterocycles: pyridones, uracils, and pyrimidinones. The synthesis and biological activities of these unique aromatic heterocyclic derivatives are reported herein. (C) 1997 Elsevier Science Ltd.
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页码:1543 / 1548
页数:6
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