Synthesis, SAR, and X-ray structure of novel potent DPPIV inhibitors: oxadiazolyl ketones

…, HJ Yim, GT Kim, HO Han, OH Kwon, TS Kwon…

Index: Koo, Ki Dong; Kim, Min Jung; Kim, Sungsub; Kim, Kyoung-Hee; Hong, Sang Yong; Hur, Gwong-Cheung; Yim, Hyeon Joo; Kim, Geun Tae; Han, Hee Oon; Kwon, O Hwan; Kwon, Tae Sik; Koh, Jong Sung; Lee, Chang-Seok Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 15 p. 4167 - 4172

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Citation Number: 14

Abstract

Synthesis of a novel series of DPPIV inhibitors with 1, 2, 4-and 1, 3, 4-oxadiazolyl ketone derivatives and its structure–activity relationships are discussed. Compound 18h showed good inhibitory activity against DPPIV and favorable pharmacokinetic properties. In vivo pharmacodynamic efficacy and co-crystal structure of compound 18h with DPPIV is also described.

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