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(3R,4S)-4-(2,4,5-Trifluorophenyl)-pyrrolidin-3-ylamine inhibitors of dipeptidyl peptidase IV: synthesis, in vitro, in vivo, and X-ray crystallographic characterization.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2007 Oct 15; Vol. 17 (20), pp. 5638-42. Date of Electronic Publication: 2007 Aug 22. - Publication Year :
- 2007
-
Abstract
- A series of pyrrolidine based inhibitors of dipeptidyl peptidase IV were developed from a high throughput screening hit for the treatment of type 2 diabetes. Potency, selectivity, and pharmacokinetic properties were optimized resulting in the identification of a pre-clinical candidate for further profiling.
- Subjects :
- Animals
Crystallography, X-Ray
Dipeptidyl Peptidase 4 chemistry
Dogs
Humans
Models, Molecular
Molecular Structure
Protease Inhibitors chemical synthesis
Protease Inhibitors pharmacokinetics
Pyrrolidines chemical synthesis
Pyrrolidines pharmacokinetics
Rats
Stereoisomerism
Dipeptidyl Peptidase 4 metabolism
Dipeptidyl-Peptidase IV Inhibitors
Fluorine chemistry
Protease Inhibitors chemistry
Protease Inhibitors pharmacology
Pyrrolidines chemistry
Pyrrolidines pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 17
- Issue :
- 20
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 17822893
- Full Text :
- https://doi.org/10.1016/j.bmcl.2007.07.081