Author/Authors :
Takashi Kondo، نويسنده , , Isamu Sugimoto، نويسنده , , Takahiro Nekado، نويسنده , , Kenya Ochi، نويسنده , , Tazumi Ohtani، نويسنده , , Yohei Tajima، نويسنده , , SUSUMU YAMAMOTO، نويسنده , , Kazuhito Kawabata، نويسنده , , Hisao Nakai، نويسنده , , Masaaki Toda، نويسنده ,
Abstract :
A 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.
