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

T Kondo, I Sugimoto, T Nekado, K Ochi, T Ohtani…

文献索引：Kondo, Takashi; Sugimoto, Isamu; Nekado, Takahiro; Ochi, Kenya; Ohtani, Tazumi; Tajima, Yohei; Yamamoto, Susumu; Kawabata, Kazuhito; Nakai, Hisao; Toda, Masaaki Bioorganic and Medicinal Chemistry, 2007 , vol. 15, # 7 p. 2715 - 2735

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被引用次数: 21

摘要

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 ...