Discovery of new chemotype dipeptidyl peptidase IV inhibitors having (R)-3-amino-3-methyl piperidine as a pharmacophore
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- 作者：Yukihiro Nishio ; Hidenori Kimura ; Shinya Tosaki ; Eiji Sugaru ; Mutsuko Sakai ; Masakuni Horiguchi ; Yumi Masui ; Michiko Ono ; Tsutomu Nakagawa ; Hiroyuki Nakahira
- 关键词：Dipeptidyl peptidase 4 ; DPP-4 ; Dipeptidyl peptidase 4 inhibitors ; DPP-4 inhibitors ; 3-Amino-piperidine ; (R)-3-Amino-3-methyl piperidine
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2010
- 出版时间：15 December 2010
- 年：2010
- 卷：20
- 期：24
- 页码：7246-7249
- 全文大小：606 K
文摘
Structures containing the (R)-3-amino-3-methyl piperidine unit as a new pharmacophore moiety have been shown to possess moderate inhibitory activity for DPP-4 with good pharmacokinetics profile. One of these compounds was found to have good oral bioavailability and PK/PD profile in ZF-rat.