1193719-40-2Relevant academic research and scientific papers
Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors
Giroux, Andre,Boulet, Louise,Brideau, Christine,Chau, Anh,Claveau, David,Cote, Bernard,Ethier, Diane,Frenette, Richard,Gagnon, Marc,Guay, Jocelyne,Guiral, Sebastien,Mancini, Joseph,Martins, Evelyn,Masse, Frederic,Methot, Nathalie,Riendeau, Denis,Rubin, Joel,Xu, Daigen,Yu, Hongping,Ducharme, Yves,Friesen, Richard W.
scheme or table, p. 5837 - 5841 (2010/04/28)
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 μM, 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
