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 1nM TAFIa inhibitor with CLT50 functional activity of 14nM but without selectivity against CPB. While not as active, aminobutyl derivative 27 provided an improved 6.7-fold selectivity for TAFIa versus CPB.
Original language | English (US) |
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Pages (from-to) | 2141-2145 |
Number of pages | 5 |
Journal | Bioorganic and Medicinal Chemistry Letters |
Volume | 14 |
Issue number | 9 |
DOIs | |
State | Published - May 3 2004 |
Externally published | Yes |
Keywords
- Carboxypeptidase
- Fibrinolysis
- TAFI
ASJC Scopus subject areas
- Biochemistry
- Molecular Medicine
- Molecular Biology
- Pharmaceutical Science
- Drug Discovery
- Clinical Biochemistry
- Organic Chemistry