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ID: ALA1137854

Journal: Bioorg Med Chem Lett

Title: Substituted piperazines as novel dipeptidyl peptidase IV inhibitors.

Authors: Brockunier LL, He J, Colwell LF, Habulihaz B, He H, Leiting B, Lyons KA, Marsilio F, Patel RA, Teffera Y, Wu JK, Thornberry NA, Weber AE, Parmee ER.

Abstract: Incorporation of a fluorophenyl beta-amino amide moiety into piperazine screening lead 2 has resulted in the discovery of a structurally novel series of potent and selective DP-IV inhibitors. Simplification of the molecule and incorporation of multiple fluorine atoms on the phenyl ring has provided low molecular weight analogs such as compound 32, which is a 19nM DP-IV inhibitor with >4000-fold selectivity over QPP.

CiteXplore: 15324904

DOI: 10.1016/j.bmcl.2004.06.065