期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 12, 页码 3565-3568出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.04.120
关键词
Azobicyclo[3.3.0]octane derivatives; Dipeptidyl peptidase 4; Oral glucose tolerance test; Type 2 diabetes mellitus
A series of novel azobicyclo[3.3.0]octane derivatives were synthesized and evaluated as dipeptidyl peptidase 4 (DPP-4) inhibitors. The effort resulted in the discovery of inhibitor 2a, which exhibited excellent efficacies in an oral glucose tolerance test. Introduction of methyl group (2j) could prolong the inhibition of serum DPP-4 activity. (C) 2010 Elsevier Ltd. All rights reserved.
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