Design and synthesis of new potent dipeptidyl peptidase IV inhibitors with enhanced ex vivo duration
详细信息 查看全文
- 作者：Takashi Kondo ; Takahiro Nekado ; Isamu Sugimoto ; Kenya Ochi ; Shigeyuki Takai ; Atsushi Kinoshita ; Yohei Tajima ; Susumu Yamamoto ; Kazuhito Kawabata ; Hisao Nakai ; et al.
- 关键词：DPP-IV inhibitor ; Prolyl-2-cyanopyrrolidine
- 刊名：Bioorganic and Medicinal Chemistry
- 出版年：2007
- 出版时间：1 April 2007
- 年：2007
- 卷：15
- 期：7
- 页码：2631-2650
- 全文大小：355 K
文摘
A series of 5β-methylprolyl-2-cyanopyrrolidine analogs were synthesized and evaluated as DPP-IV inhibitors, and the duration of their ex vivo activity was assessed. Comparison of their potency and duration of action was done among three different species. The mode of binding was investigated, and the effect on the plasma glucose level was evaluated. Structure–activity relationships are also presented.