Design, synthesis and biological evaluation of benzo [1.3. 2] dithiazolium ylide 1, 1-dioxide derivatives as potential dual cyclooxygenase-2/5-lipoxygenase inhibitors

…, GS Chen, CS Chen, PT Chang, JW Chern

Index: Tan, Chen-Ming; Chen, Grace Shiahuy; Chen, Chien-Shu; Chang, Pei-Teh; Chern, Ji-Wang Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 21 p. 6316 - 6328

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Citation Number: 5

Abstract

3-(4-Bromophenyl)-6-nitrobenzo [1.3. 2] dithiazolium ylide 1, 1-dioxide (5) was discovered as a new prototype for dual inhibitors of cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5- LOX). Thus, the structure–activity relationships of benzo [1.3. 2] dithiazolium ylide 1, 1- dioxide skeleton were carried out. The 6-NO2 group played an essential role in the inhibitory activity. In addition, moderate-sized lipophilic substituents at the para-position of the 3-aryl ...