Abstract
A new type of 1-aryl-5-(4-methylsulfonylphenyl)imidazoles, possessing C-2 alkylthio (SMe or SEt) substituents, were designed and synthesized for evaluation as selective cyclooxygenase-2 (COX-2) inhibitors with in vivo anti-inflammatory activity. The compound, 1-(4-bromophenyl)-5-(4-methylsulfonylphenyl)-2-methylthioimidazole ( 11g), was the most potent and selective COX-2 inhibitor (COX-2 IC 50 = 0.43 μM with no inhibition of COX-1 up to 25 μM) relative to the reference drug celecoxib (COX-2 IC 50 = 0.21 μM with no inhibition of COX-1 up to 25 μM) and also showed very good anti-inflammatory activity compared to celecoxib in carrageenan-induced rat paw edema assay.
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