期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 14, 期 18, 页码 4759-4762出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2004.06.099
关键词
DP-IV
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 (IC50=270, 119nM, respectively). (C) 2004 Elsevier Ltd. All rights reserved.
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