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

Authors :
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
Source :
Bioorganic & Medicinal Chemistry Letters. Aug2007, Vol. 17 Issue 15, p4167-4172. 6p.
Publication Year :
2007

Abstract

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. [Copyright &y& Elsevier]

Details

Language :
English
ISSN :
0960894X
Volume :
17
Issue :
15
Database :
Academic Search Index
Journal :
Bioorganic & Medicinal Chemistry Letters
Publication Type :
Academic Journal
Accession number :
25618637
Full Text :
https://doi.org/10.1016/j.bmcl.2007.05.046