Title of article
Discovery of potent and selective β-homophenylalanine based dipeptidyl peptidase IV inhibitors
Author/Authors
Jinyou Xu، نويسنده , , Hyun O. Ok، نويسنده , , Edward J. Gonzalez، نويسنده , , Lawrence F. Colwell Jr.، نويسنده , , Bahanu Habulihaz، نويسنده , , Huaibing He، نويسنده , , Barbara Leiting، نويسنده , , Kathryn A. Lyons، نويسنده , , Frank Marsilio، نويسنده , , Reshma A. Patel، نويسنده , , Joseph K. Wu، نويسنده , , Nancy A. Thornberry، نويسنده , , Ann E. Weber، نويسنده , , Emma R. Parmee، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2004
Pages
4
From page
4759
To page
4762
Abstract
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).
Keywords
DP-IV.* Corresponding author. Tel.: +1-732-594-2217 , e-mail: jinyou_xu@merck.com , fax: +1-732-594-5790
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2004
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
794869
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