Synthesis, biological evaluation and structural determination of beta-aminoacyl-containing cyclic hydrazine derivatives as dipeptidlyl peptidase IV (DPP-IV) inhibitors

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Inhibitors of dipeptidyl peptidase IV (DPP-IV) have been shown to be effective treatments for type 2 diabetes. A series of 0-aminoacyl-containing cyclic hydrazine derivatives were synthesized and evaluated as DPP-IV inhibitors. One member of this series, (R)-3 -amino-1-(2-benzoyl-1, 2-diazepan-1-yl)-4-(2,4,5-trifluorophenyl)butan-1-one (10f), showed potent in vitro activity, good selectivity and in vivo efficacy in mouse models. Also, the binding mode of compound 10f was determined by X-ray crystallography. (c) 2007 Elsevier Ltd. All rights reserved.
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Issue Date
2007-05
Language
English
Article Type
Article
Keywords

GLUCAGON-LIKE PEPTIDE-1; TYPE-2 DIABETES-MELLITUS; PYRAZOLIDINE DERIVATIVES; GLUCOSE-TOLERANCE; INSULIN-SECRETION; POTENT; MICE

Citation

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.17, no.9, pp.2622 - 2628

ISSN
0960-894X
DOI
10.1016/j.bmcl.2007.01.111
URI
http://hdl.handle.net/10203/11147
Appears in Collection
CH-Journal Papers(저널논문)
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