Diaryl indenes and benzofurans: Novel classes of potent and selective cyclooxygenase-2 inhibitors

Novel series of diaryl indenes and benzofurans have been shown to be potent and selective COX-2 inhibitors. A structure-activity relationship study suggests that the conversion of sulfones to sulfonamides affords potent, but slightly less selective COX-2 inhibitors, and that for benzofurans the 3-ha...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1995-10, Vol.5 (20), p.2377-2380
Main Authors: Huang, Horng-Chih, Chamberlain, Timothy S., Selbert, Karen, Koboldt, Carol M., Isakson, Peter C., Reitz, David B.
Format: Article
Language:English
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Summary:Novel series of diaryl indenes and benzofurans have been shown to be potent and selective COX-2 inhibitors. A structure-activity relationship study suggests that the conversion of sulfones to sulfonamides affords potent, but slightly less selective COX-2 inhibitors, and that for benzofurans the 3-halo-4-methoxyphenyl sulfonamide analogs are more selective than the corresponding 4-fluorophenyl analog. Novel series of diaryl indenes and benzofurans have been shown to be potent and selective COX-2 inhibitors. The conversion of sulfones to sulfonamides affords potent, but slightly less selective COX-2 inhibitors. For benzofurans, the 3-halo-4-methoxyphenyl sulfonamide analogs are more selective than the 4-fluorophenyl analog.
ISSN:0960-894X
1464-3405
DOI:10.1016/0960-894X(95)00414-O