Discovery of potent, selective, and orally bioavailable quinoline-based dipeptidyl peptidase IV inhibitors targeting Lys554.

Hironobu Maezaki,Yoshihiro Banno,Yasufumi Miyamoto,Yusuke Moritoh, Yuusuke Moritou,Tomoko Asakawa,Osamu Kataoka,Koji Takeuchi,Nobuhiro Suzuki,Koji Ikedo,Takuo Kosaka,Masako Sasaki,Shigetoshi Tsubotani,Akiyoshi Tani,Miyuki Funami,Yoshio Yamamoto,Michiko Tawada,Kathleen Aertgeerts,Jason Yano,Satoru Oi

Bioorganic & Medicinal Chemistry（2011）

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摘要

A novel series of quinoline-based dipeptidyl peptidase IV inhibitors were designed based on the co-crystallography and synthesized to target the side chain of Lys554 on the enzyme.

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关键词

DPP-4,T2DM,GLP-1,SAR,SBDD,Boc,TBS,Cbz,ADME,F,CLtotal,Vdss

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