Diarylspiro [2.4] heptenes as orally active, highly selective cyclooxygenase-2 inhibitors: synthesis and structure-activity relationships
…, GD Anderson, AW Veenhuizen, Y Zhang…
Index: Huang, Horng-Chih; Li, James J.; Garland, Danny J.; Chamberlain, Timothy S.; Reinhard, Emily J.; Manning, Robert E.; Seibert, Karen; Koboldt, Carol M.; Gregory, Susan A.; Anderson, Gary D.; Veenhuizen, Amy W.; Zhang, Yan; Perkins, William E.; Burton, Earl G.; Cogburn, J. Nita; Isakson, Peter C.; Reitz, David B. Journal of Medicinal Chemistry, 1996 , vol. 39, # 1 p. 253 - 266
Full Text: HTML
Citation Number: 59
Abstract
A novel series of 5, 6-diarylspiro [2.4] hept-5-enes was shown to provide highly potent and selective cyclooxygenase-2 (COX-2) inhibitors. A study of structure-activity relationships in this series suggests that 3, 4-disubstituted phenyl analogs are generally more selective than 4-substituted phenyl analogs and that replacement of the methyl sulfone group on the 6- phenyl ring with a sulfonamide moiety results in compounds with superior in vivo ...
Related Articles:
[Liu, Gai-Zhi; Xu, Hai-Wei; Wang, Peng; Lin, Zong-Tao; Duan, Ying-Chao; Zheng, Jia-Xin; Liu, Hong-Min European Journal of Medicinal Chemistry, 2013 , vol. 65, p. 323 - 336]
[Liu, Gai-Zhi; Xu, Hai-Wei; Wang, Peng; Lin, Zong-Tao; Duan, Ying-Chao; Zheng, Jia-Xin; Liu, Hong-Min European Journal of Medicinal Chemistry, 2013 , vol. 65, p. 323 - 336]
[Liu, Gai-Zhi; Xu, Hai-Wei; Wang, Peng; Lin, Zong-Tao; Duan, Ying-Chao; Zheng, Jia-Xin; Liu, Hong-Min European Journal of Medicinal Chemistry, 2013 , vol. 65, p. 323 - 336]
[Wuest, Frank R.; Hoehne, Aileen; Metz, Peter Organic and Biomolecular Chemistry, 2005 , vol. 3, # 3 p. 503 - 507]
[Wuest, Frank R.; Hoehne, Aileen; Metz, Peter Organic and Biomolecular Chemistry, 2005 , vol. 3, # 3 p. 503 - 507]