期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 17, 期 7, 页码 1903-1907出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2007.01.039
关键词
type 2 diabetes; DPP-IV inhibitors; 1,4-diazepan-2-one
Following the discovery of N-acyl-1,4-diazepan-2-one as a novel pharmacophore for potent and selective DPP-4 inhibitors, optimization of this new lead with different substitution on the seven-membered ring resulted in several highly potent and selective, orally bioavailable, and efficacious DPP-4 inhibitors, such as 3R-methyl-1-cyclopropyl-1,4-diazepan-2-one derivative 9i (DPP-4 IC50 = 8.0 nM) and 3R,6R-dimethyl-1,4-diazepan-2-one derivative 14a (DPP-4 IC50 = 9.7 nM). (c) 2007 Elsevier Ltd. All rights reserved.
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