| Literature DB >> 15324903 |
Jinyou Xu1, Hyun O Ok, Edward J Gonzalez, Lawrence F Colwell, Bahanu Habulihaz, Huaibing He, Barbara Leiting, Kathryn A Lyons, Frank Marsilio, Reshma A Patel, Joseph K Wu, Nancy A Thornberry, Ann E Weber, Emma R Parmee.
Abstract
Modification of in-house screening lead beta-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 (IC(50)=270, 119nM, respectively).Entities:
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Year: 2004 PMID： 15324903 DOI： 10.1016/j.bmcl.2004.06.099
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823