Abstract
Novel dipeptidyl peptidase IV (DPP-IV) inhibitors with a phenethylphenylphthalimide skeleton were prepared based on α-glucosidase inhibitors and liver X receptor (LXR) antagonists derived from thalidomide. Representative compounds showed non-competitive inhibition of DPP-IV and 28a exhibited 10-fold selectivity for DPP-IV over DPP-8. Compound 28a is the first non-competitive, selective DPP-IV inhibitor.
Original language | English |
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Pages (from-to) | 3041-3045 |
Number of pages | 5 |
Journal | Bioorganic and Medicinal Chemistry Letters |
Volume | 21 |
Issue number | 10 |
DOIs | |
Publication status | Published - 2011 May 15 |
Externally published | Yes |
Keywords
- Dipeptidyl peptidase IV
- Enzyme inhibitor
- Non-competitive inhibition
- Phthalimide
- Subtype selectivity
ASJC Scopus subject areas
- Biochemistry
- Molecular Medicine
- Molecular Biology
- Pharmaceutical Science
- Drug Discovery
- Clinical Biochemistry
- Organic Chemistry