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Bioorg Med Chem Lett. 2004 May 3;14(9):2141-5.

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

Author information

1
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, West Point, PA 19486, USA. philippe_nantermet@merck.com

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.

PMID:
15080996
DOI:
10.1016/j.bmcl.2004.02.033
[Indexed for MEDLINE]

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