Discovery of potent, selective, and orally bioavailable pyridone-based dipeptidyl peptidase-4 inhibitors.

Jinyou Xu,Lan Wei,Robert Mathvink,Scott D Edmondson,Anthony Mastracchio,George J Eiermann,Huaibing He,Joseph F Leone,Barbara Leiting,Kathryn A Lyons,Frank Marsilio,Reshma A Patel,Aleksandr Petrov,Joseph K Wu,Nancy A Thornberry,Ann E Weber

Bioorganic & Medicinal Chemistry Letters（2006）

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摘要

anti-Substituted biaryl β-methylphenylalanine derived amides have been shown to be potent DPP-4 inhibitors exhibiting excellent selectivity over both DPP8 and DPP9. The optimized compound 9 exhibited good pharmacokinetic profiles in three preclinical species.

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DPP-4 inhibitors

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