Synthesis and pharmacological characterization of potent, selective, and orally bioavailable isoindoline class dipeptidyl peptidase IV inhibitors

نویسندگان

  • Noriyasu Kato
  • Mitsuru Oka
  • Takayo Murase
  • Masahiro Yoshida
  • Masao Sakairi
  • Mirensha Yakufu
  • Satoko Yamashita
  • Yoshika Yasuda
  • Aya Yoshikawa
  • Yuji Hayashi
  • Masahiro Shirai
  • Yukie Mizuno
  • Mitsuaki Takeuchi
  • Mitsuhiro Makino
  • Motohiro Takeda
  • Takuji Kakigami
چکیده

Focused structure-activity relationships of isoindoline class DPP-IV inhibitors have led to the discovery of 4b as a highly selective, potent inhibitor of DPP-IV. In vivo studies in Wistar/ST rats showed that 4b was converted into the strongly active metabolite 4l in high yield, resulting in good in vivo efficacy for antihyperglycemic activity.

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عنوان ژورنال:

دوره 1  شماره 

صفحات  -

تاریخ انتشار 2011