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Bioorg Med Chem Lett. 2008 Apr 1;18(7):2409-13. doi: 10.1016/j.bmcl.2008.02.050. Epub 2008 Feb 26.

Fluoroolefins as amide bond mimics in dipeptidyl peptidase IV inhibitors.

Author information

1
Department of Medicinal Chemistry, Merck & Co. Inc., PO Box 2000, Rahway, NJ 07065, USA. scott_edmondson@merck.com

Abstract

The synthesis, selectivity, rat pharmacokinetic profile, and drug metabolism profiles of a series of potent fluoroolefin-derived DPP-4 inhibitors (4) are reported. A radiolabeled fluoroolefin 33 was shown to possess a high propensity to form reactive metabolites, thus revealing a potential liability for this class of DPP-4 inhibitors.

PMID:
18331795
DOI:
10.1016/j.bmcl.2008.02.050
[Indexed for MEDLINE]

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