| 15324904 |
Brockunier LL, He J, Colwell LF Jr, Habulihaz B, He H, Leiting B, Lyons KA, Marsilio F, Patel RA, Teffera Y, Wu JK, Thornberry NA, Weber AE, Parmee ER: Substituted piperazines as novel dipeptidyl peptidase IV inhibitors. . Bioorg Med Chem Lett. 2004 Sep 20;14(18):4763-6.
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. |
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