4.5 Article

Potent non-nitrile dipeptidic dipeptidyl peptidase IV inhibitors

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 17, Issue 23, Pages 6476-6480

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2007.09.090

Keywords

DPP4; serine protease; diabetes; non-nitrile; GLP-1

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The synthesis and structure- activity relationships of novel dipeptidyl peptidase IV inhibitors replacing the classical cyanopyrrolidine P1 group with other small nitrogen heterocycles are described. A unique potency enhancement was achieved with beta-branched natural and unnatural amino acids, particularly adamantylglycines, linked to a (2S, 3R)-2,3-methanopyrrolidine based scaffold. (c) 2007 Elsevier Ltd. All rights reserved.

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