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This document describes a study that synthesized and tested a group of 1-(aminosulfonylphenyl and methylsulfonylphenyl)-2-(pyridyl)acetylene regioisomers as COX-1 and COX-2 inhibitors. The position of the COX-2 SO2NH2 or SO2Me pharmacophore on the phenyl ring and the attachment point of the pyridyl ring were found to impact inhibitory potency and selectivity. Several compounds exhibited potent and highly selective COX-2 inhibition, including 1-(4-aminosulfonylphenyl)-2-(3-methyl-2-pyridyl)acetylene, with an

Author

Fx Hendrick Sebastian

Language

EN