Title of article
Imidazole acetic acid TAFIa inhibitors: SAR studies centered around the basic P1′ group
Author/Authors
Philippe G. Nantermet، نويسنده , , James C. Barrow، نويسنده , , Stacey R Lindsley، نويسنده , , MaryBeth Young، نويسنده , , Shi-Shan Mao، نويسنده , , Steven Carroll، نويسنده , , Carolyn Bailey، نويسنده , , Michele Bosserman، نويسنده , , Dennis Colussi، نويسنده , , Daniel R. McMasters، نويسنده , , Joseph P Vacca، نويسنده , , Harold G. Selnick، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2004
Pages
5
From page
2141
To page
2145
Abstract
Structural modifications of the aminopyridine P1′ group of imidazole acetic acid based TAFIa inhibitors led to the discovery of the aminocyclopentyl analog 28, a 1 nM TAFIa inhibitor with CLT50 functional activity of 14 nM but without selectivity against CPB. While not as active, aminobutyl derivative 27 provided an improved 6.7-fold selectivity for TAFIa versus CPB.
Keywords
TAFI , Carboxypeptidase.* Correspondingauthor. Tel.: +1-215-6520945 , fax: +1-215-6523971 , e-mail: philippe_nantermet@merck.com , fibrinolysis
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2004
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
794355
Link To Document