- Discovery of potent and selective β-homophenylalanine based dipeptidyl peptidase IV inhibitors
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Modification of in-house screening lead β-aminoacyl proline 8 gave an equipotent thiazolidide 9. Extensive SAR studies on the phenyl ring of 9 led to the discovery of a novel series of potent and selective DP-IV inhibitors. Introduction of a fluorine at the 2-position proved to be crucial for the potency of this series. The 2,5-difluoro (22q) and 2,4,5-trifluoro (22t) analogues were potent inhibitors of DP-IV (IC50 = 270, 119 nM, respectively).
- Xu, Jinyou,Ok, Hyun O.,Gonzalez, Edward J.,Colwell Jr., Lawrence F.,Habulihaz, Bahanu,He, Huaibing,Leiting, Barbara,Lyons, Kathryn A.,Marsilio, Frank,Patel, Reshma A.,Wu, Joseph K.,Thornberry, Nancy A.,Weber, Ann E.,Parmee, Emma R.
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p. 4759 - 4762
(2007/10/03)
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