期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 20, 页码 5837-5841出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.08.085
关键词
mPGES-1; Inhibitors; Phenanthrene imidazole; Activity; Pharmacokinetic
Phenanthrene imidazoles 26 and 44 have been identified as novel potent, selective and orally active mPGES-1 inhibitors. These inhibitors are significantly more potent than the previously reported chlorophenanthrene imidazole 1 (MF63) with a human whole blood IC50 of 0.20 and 0.14 mu M, respectively. It exhibited a significant analgesic effect in a guinea pig hyperalgesia model at oral doses as low as 14 mg/kg. Both active and selective mPGES-1 inhibitors (26 and 44) have a relatively distinct pharmacokinetic profile and are suitable for clinical development. Crown Copyright (C) 2009 Published by Elsevier Ltd. All rights reserved.
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