Development of new non-peptide GPIIb/IIIa antagonists, NSL-95315 and NSL-95317, isosteres of NSL-95300

被引：8

作者：

Asari, T

Ishikawa, S

Sasaki, T

Katada, J

Hayashi, Y

Harada, T

Yano, M

Yasuda, E

Uno, I

Ojima, I

机构：

[1] NIPPON STEEL CORP LTD,LIFE SCI RES CTR,ADV TECHNOL RES LABS,NAKAHARA KU,KAWASAKI,KANAGAWA 211,JAPAN

[2] SUNY STONY BROOK,DEPT CHEM,STONY BROOK,NY 11794

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 16期

关键词：

D O I：

10.1016/S0960-894X(97)00366-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthetic and structure-activity relationship (SAR) studies of new non-peptide GPIIb/IIIa antagonists (1a-f and 3) were conducted by replacing one amide bond of NSL-95300 (2) with an (E)-double bond or an enone group. NSL-95315 (1a) and NSL-95317 (3) showed the inhibitory activity for collagen-induced human platelet aggregation with IC50 values of 0.25 mu M and 0.21 mu M, respectively. (C) 1997 Elsevier Science Ltd.

引用

页码：2099 / 2104

页数：6

共 17 条

[1]

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

[2]

Dickerson R. E., 1969, STRUCTURE ACTION PRO, P13

[3]

HAFFAR BM, 1991, J BIOL CHEM, V266, P316

[4] DOUBLE-BOND ISOSTERES OF THE PEPTIDE-BOND - ENKEPHALIN ANALOG [J].