Discovery of new chemotype dipeptidyl peptidase IV inhibitors having (R)-3-amino-3-methyl piperidine as a pharmacophore

Y Nishio, H Kimura, S Tosaki, E Sugaru, M Sakai…

文献索引：Nishio, Yukihiro; Kimura, Hidenori; Tosaki, Shinya; Sugaru, Eiji; Sakai, Mutsuko; Horiguchi, Masakuni; Masui, Yumi; Ono, Michiko; Nakagawa, Tsutomu; Nakahira, Hiroyuki Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 24 p. 7246 - 7249

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被引用次数: 16

摘要

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.