DESIGN, SYNTHESIS AND BIOLOGICAL-ACTIVITY OF NOVEL RIGID AMIDINO-PHENYLALANINE DERIVATIVES AS INHIBITORS OF THROMBIN

被引：23

作者：

MACK, H ^{[1
]}

PFEIFFER, T ^{[1
]}

HORNBERGER, W ^{[1
]}

BOHM, HJ ^{[1
]}

HOFFKEN, HW ^{[1
]}

机构：

[1] BASF AG,DEPT ANGIOL,KNOLL,D-67056 LUDWIGSHAFEN,GERMANY

来源：

JOURNAL OF ENZYME INHIBITION | 1995年 / 9卷 / 01期

关键词：

THROMBIN; INHIBITOR; COAGULATION;

D O I：

10.3109/14756369509040682

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

(3S)-(Naphthalene-2-sulfonylamino)-1-[2R-(4-amidinophenyl)-1- piperidinocarbonylethyl]-2-pyrrolidinone (1a) is a potent inhibitor of thrombin with an IC50 value by 112 times lower than that of NAPAP (racemate). The selectivity versus trypsin can be improved by incorporation of substituents on the naphthyl ring. The mode of binding of the compound was determined by X-ray crystallography.

引用

页码：73 / &

共 12 条

[1] REFINED 2.3-ANGSTROM X-RAY CRYSTAL-STRUCTURE OF BOVINE THROMBIN COMPLEXES FORMED WITH THE BENZAMIDINE AND ARGININE-BASED THROMBIN INHIBITORS NAPAP, 4-TAPAP AND MQPA - A STARTING POINT FOR IMPROVING ANTITHROMBOTICS [J].