479586-00-0Relevant academic research and scientific papers
Discovery of potent and selective β-homophenylalanine based dipeptidyl peptidase IV inhibitors
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.
, p. 4759 - 4762 (2007/10/03)
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).
