| Literature DB >> 17292611 |
Takashi Kondo1, Isamu Sugimoto, Takahiro Nekado, Kenya Ochi, Tazumi Ohtani, Yohei Tajima, Susumu Yamamoto, Kazuhito Kawabata, Hisao Nakai, Masaaki Toda.
Abstract
A series of (4-substituted prolyl)prolinenitriles were synthesized and evaluated as inhibitors of dipeptidylpeptidase IV (DPP-IV). Among those tested, the 4beta-[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.Entities:
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Year: 2007 PMID： 17292611 DOI： 10.1016/j.bmc.2007.01.033
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641