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Cyclooxygenase-2 inhibitors. Synthesis and pharmacological activities of 5-methanesulfonamido-1-indanone derivatives

…, AW Ford-Hutchinson, JY Gauthier…

文献索引:Li; Black; Chan; Ford-Hutchinson; Gauthier; Gordon; Guay; Kargman; Lau; Mancini; Ouimet; Roy; Vickers; Wong; Young; Zamboni; Prasit Journal of Medicinal Chemistry, 1995 , vol. 38, # 25 p. 4897 - 4905

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被引用次数: 74

摘要

COX-2 inhibitor. The structure-activity relationships in this series have been extensively studied. Ortho-and para-substituted 6-phenyl substitutents are optimal for in vitro potency. Replacement of this phenyl ring by a variety of heterocycles gave compounds that were less active. The methanesulfonamido group seems to be the optimal group at the 5-position of the indanone system. Compound 20 has an efficacy profile that is superior or comparable ...