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Design and synthesis of long-acting inhibitors of dipeptidyl peptidase IV

Takashi Kondo - No affiliation found

2007/04/01 Full-length article DOI: 10.1016/j.bmc.2007.01.033 Journal: Bioorganic & Medicinal Chemistry

Abstract:

AbstractA series of (4-substituted prolyl)prolinenitriles were synthesized and evaluated as inhibitors of dipeptidylpeptidase IV (DPP-IV). Among those tested, the 4β-[4-(hydroxyphenyl)prolyl]prolinenitriles showed a potent inhibitory activity with a long duration of action. Metabolic formation of the corresponding phenol glucuronates was found to contribute to their long duration of action. The activity profiles of the synthesized compounds are reported and structure–activity relationships are also presented.