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Discovery of new chemotype dipeptidyl peptidase IV inhibitors having (R)-3-amino-3-methyl piperidine as a pharmacophore.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2010 Dec 15; Vol. 20 (24), pp. 7246-9. Date of Electronic Publication: 2010 Oct 26. - Publication Year :
- 2010
-
Abstract
- Structures containing the (R)-3-amino-3-methyl piperidine unit as a new pharmacophore moiety have been shown to possess moderate inhibitory activity for DPP-4 with good pharmacokinetics profile. One of these compounds was found to have good oral bioavailability and PK/PD profile in ZF-rat.<br /> (Copyright © 2010 Elsevier Ltd. All rights reserved.)
- Subjects :
- Animals
Dipeptidyl Peptidase 4 metabolism
Dipeptidyl-Peptidase IV Inhibitors chemical synthesis
Dipeptidyl-Peptidase IV Inhibitors pharmacokinetics
Drug Evaluation, Preclinical
Humans
Microsomes, Liver metabolism
Piperidines chemical synthesis
Piperidines pharmacokinetics
Pyrimidinones chemical synthesis
Pyrimidinones pharmacokinetics
Rats
Stereoisomerism
Structure-Activity Relationship
Dipeptidyl Peptidase 4 chemistry
Dipeptidyl-Peptidase IV Inhibitors chemistry
Piperidines chemistry
Pyrimidinones chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 20
- Issue :
- 24
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 21074430
- Full Text :
- https://doi.org/10.1016/j.bmcl.2010.10.101