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A novel series of [4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)-2-pyrimidine-based cyclooxygenase-2 (COX-2) inhibitors, which have a different arrangement of substituents compared to the more common 1,2-diarylheterocycle based molecules, have been discovered. For example, 2-(butyloxy)-4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)pyrimidine (47), a member of the 2-pyrimidinyl ether series, has been shown to be a potent and selective inhibitor with a favourable pharmacokinetic profile, high brain penetration and good efficacy in rat models of hypersensitivity.

Original publication

DOI

10.1016/j.bmcl.2009.02.085

Type

Journal article

Journal

Bioorg Med Chem Lett

Publication Date

01/08/2009

Volume

19

Pages

4504 - 4508

Keywords

Amines, Animals, Brain, Chemistry, Pharmaceutical, Cyclooxygenase 2, Cyclooxygenase 2 Inhibitors, Disease Models, Animal, Drug Design, Ethers, Humans, Inflammation, Inhibitory Concentration 50, Mice, Molecular Structure, Neurodegenerative Diseases, Pyrimidines, Rats, Sulfones