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Bioorg Med Chem Lett. 2007 Dec 1;17(23):6476-80. Epub 2007 Oct 1.

Potent non-nitrile dipeptidic dipeptidyl peptidase IV inhibitors.

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  • 1Bristol-Myers Squibb Research and Development, PO Box 5400, Princeton, NJ 08543-5400, USA.

Abstract

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.

PMID:
17937986
DOI:
10.1016/j.bmcl.2007.09.090
[PubMed - indexed for MEDLINE]

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