Synthesis and biological evaluation of linear phenylethynylbenzenesulfonamide regioisomers as cyclooxygenase-1/-2 (COX-1/-2) inhibitors

R Anana, PNP Rao, QH Chen, EE Knaus

文献索引：Anana, Raymond; Rao, P.N. Praveen; Chen, Qiao-Hong; Knaus, Edward E. Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 15 p. 5259 - 5265

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被引用次数: 23

摘要

A group of regioisomeric phenylethynylbenzenesulfonamides possessing a COX-2 SO2NH2 pharmacophore at the para-, meta-or ortho-position of the C-1 phenyl ring, in conjunction with a C-2 substituted-phenyl (H, OMe, OH, Me, F) group, were synthesized and evaluated as inhibitors of the cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) isozymes. The target 1, 2-diphenylacetylenes were synthesized via a palladium-catalyzed ...