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Imidazole acetic acid TAFIa inhibitors: SAR studies centered around the basic P(1)(') group.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2004 May 03; Vol. 14 (9), pp. 2141-5. - Publication Year :
- 2004
-
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.
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 14
- Issue :
- 9
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 15080996
- Full Text :
- https://doi.org/10.1016/j.bmcl.2004.02.033