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Synthesis and cyclooxygenase inhibition of various (aryl-1, 2, 3-triazole-1-yl)-methanesulfonylphenyl derivatives

…, X Tang, T Kniess, J Pietzsch, M Suresh

文献索引:Wuest, Frank; Tang, Xinli; Kniess, Torsten; Pietzsch, Jens; Suresh, Mavanur Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 3 p. 1146 - 1151

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被引用次数: 42

摘要

A series of 1, 4-and 1, 5-diaryl substituted 1, 2, 3-triazoles was synthesized by either Cu (I)- catalyzed or Ru (II)-catalyzed 1, 3-dipolar cycloaddition reactions between 1-azido-4- methane-sulfonylbenzene 9 and a panel of various para-substituted phenyl acetylenes (4-H, 4-Me, 4-OMe, 4-NMe2, 4-Cl, 4-F). All compounds were used in in vitro cyclooxygenase (COX) assays to determine the combined electronic and steric effects upon COX-1 and ...