Inhibition of FAP
- Deposit:2011-09-18
- Modify:2018-09-17
Title: Synthesis and evaluation of [(1R)-1-amino-2-(2,5-difluorophenyl)ethyl]cyclohexanes and 4-[(1R)-1-amino-2-(2,5-difluorophenyl)ethyl]piperidines as DPP-4 inhibitors.
Abstract: A series of 4-amino cyclohexanes and 4-substituted piperidines were prepared and evaluated for inhibition of DPP-4. Analog 20q displayed both good DPP-4 potency and selectivity against other proteases, while derivative 20k displayed long half life and modest oral bioavailability in rat. The most potent analog, 3-(5-aminocarbonylpyridyl piperidine 53j, displayed excellent DPP-4 activity with good selectivity versus other proline enzymes.
Journal: Bioorg Med Chem Lett
Year: 2011
Volume: 21
Issue: 6
First Page: 1880
Last Page: 1886
DOI: 10.1016/j.bmcl.2010.12.060
Target ChEMBL ID: CHEMBL4683
ChEMBL Target Name: Fibroblast activation protein alpha
ChEMBL Target Type: SINGLE PROTEIN - Target is a single protein chain
Relationship Type: H - Homologous protein target assigned
Confidence: Homologous single protein target assigned
- PubChem
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