Bioorganic and Medicinal Chemistry Letters p. 2409 - 2413 (2008)
Update date:2022-08-04
Topics:
Edmondson, Scott D.
Wei, Lan
Xu, Jinyou
Shang, Jackie
Xu, Shiyao
Pang, Jianmei
Chaudhary, Ashok
Dean, Dennis C.
He, Huaibing
Leiting, Barbara
Lyons, Kathryn A.
Patel, Reshma A.
Patel, Sangita B.
Scapin, Giovanna
Wu, Joseph K.
Beconi, Maria G.
Thornberry, Nancy A.
Weber, Ann E.
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.
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(2008)
