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

Autor:	Chang Seok Lee, Geun Tae Kim, Min-Jung Kim, Sang Yong Hong, Hee Oon Han, Gwong-Cheung Hur, O Hwan Kwon, Kyoung-Hee Kim, Sungsub Kim, Jong Sung Koh, Ki Dong Koo, Hyeon Joo Yim, Tae Sik Kwon
Rok vydání:	2007
Předmět:	Models Molecular Ketone Stereochemistry Dipeptidyl Peptidase 4 Clinical Biochemistry Pharmaceutical Science Crystallography X-Ray Biochemistry Chemical synthesis Structure-Activity Relationship Dogs In vivo Drug Discovery Hydrolase Animals Protease Inhibitors Molecular Biology Dipeptidyl peptidase-4 chemistry.chemical_classification Dipeptidyl-Peptidase IV Inhibitors Molecular Structure biology Organic Chemistry Haplorhini Ketones In vitro Rats Kinetics Enzyme chemistry Enzyme inhibitor biology.protein Molecular Medicine
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 17:4167-4172
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2007.05.046
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7a9292fe70f399944b3adad2316c5fd0 https://doi.org/10.1016/j.bmcl.2007.05.046 Zobrazit plný text záznamu Full Text from ScienceDirect