期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 18, 期 11, 页码 3200-3205出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.04.064
关键词
quinoline/naphthalene-difluoromethylphosphonate; PTP1B inhibitors; diabetes; obesity; cancer
A series of quinoline/naphthalene-difluoromethylphosphonates were prepared and were found to be potent PTP1B inhibitors. Most of these compounds bearing polar functionalities or large lipophilic residues did not show appreciable oral bioavailability in rodents while small and less polar analogs displayed moderate to good oral bioavailability. The title compound was found to have the best overall potency and pharmacokinetic pro. le and was found to be efficacious in animal models of diabetes and cancer. (C) 2008 Elsevier Ltd. All rights reserved.
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