Syntheses and characterization of nimesulide derivatives for dual enzyme inhibitors of both cyclooxygenase-1/2 and 5-lipoxygenase

Y Li, SH Chen, TM Ou, JH Tan, D Li, LQ Gu…

Index: Li, Yue; Chen, Shu-Han; Ou, Tian-Miao; Tan, Jia-Heng; Li, Ding; Gu, Lian-Quan; Huang, Zhi-Shu Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 6 p. 2074 - 2083

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Citation Number: 12

Abstract

Cyclooxygenase-1/2 (COX-1/2) and 5-lipoxygenase (5-LOX) are enzymes in two different pathways in the inflammatory process. In the present study, a variety of new nimesulide derivatives were synthesized through incorporation of a 5-LOX pharmacophore into nimesulide followed with some structural modifications, which were then characterized for dual enzyme inhibitors for these two types of enzymes. Their structure–activity ...