Imidazole acetic acid TAFIa inhibitors: SAR studies centered around the basic P(1)(') group.

Research paper by Philippe G PG Nantermet, James C JC Barrow, Stacey R SR Lindsley, MaryBeth M Young, Shi-Shan SS Mao, Steven S Carroll, Carolyn C Bailey, Michele M Bosserman, Dennis D Colussi, Daniel R DR McMasters, Joseph P JP Vacca, Harold G HG Selnick

Indexed on: 15 Apr '04Published on: 15 Apr '04Published in: Bioorganic & Medicinal Chemistry Letters

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Abstract

Structural modifications of the aminopyridine P(1)(') group of imidazole acetic acid based TAFIa inhibitors led to the discovery of the aminocyclopentyl analog 28, a 1 nM TAFIa inhibitor with CLT(50) 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.

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