| Literature DB >> 14684294 |
Emma R Parmee1, Jiafang He, Anthony Mastracchio, Scott D Edmondson, Larry Colwell, George Eiermann, William P Feeney, Bahanu Habulihaz, Huaibing He, Ruth Kilburn, Barbara Leiting, Kathryn Lyons, Frank Marsilio, Reshma A Patel, Aleksandr Petrov, Jerry Di Salvo, Joseph K Wu, Nancy A Thornberry, Ann E Weber.
Abstract
Substituted 4-amino cyclohexylglycine analogues were evaluated for DP-IV inhibitory properties. Bis-sulfonamide 15e was an extremely potent 2.6 nM inhibitor of the enzyme with excellent selectivity over all counterscreens. 2,4-difluorobenzenesulfonamide 15b and 1-naphthyl amide 16b, however, combined an acceptable in vitro profile with good pharmacokinetic properties in the rat, and 15b was orally efficacious at 3 mpk in an OGTT in lean mice.Entities:
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Year: 2004 PMID： 14684294 DOI： 10.1016/j.bmcl.2003.10.016
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823