Discovery of potential anti-inflammatory drugs: diaryl-1, 2, 4-triazoles bearing N-hydroxyurea moiety as dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase

…, H Yao, J Jiang, X Wu, S Jiang, Q Wang, T Lu…

Index: Jiang, Bo; Huang, Xiaojing; Yao, Hequan; Jiang, Jieyun; Wu, Xiaoming; Jiang, Siyi; Wang, Qiujuan; Lu, Tao; Xu, Jinyi Organic and Biomolecular Chemistry, 2014 , vol. 12, # 13 p. 2114 - 2127

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Citation Number: 17

Abstract

A series of hybrids from diaryl-1, 2, 4-triazole and hydroxamic acid or N-hydroxyurea were synthesized and evaluated as novel anti-inflammatory agents. The biological data showed that (i) all the compounds showed dual COX-2/5-LOX inhibitory activities in vitro, and 15e showed optimal inhibitory activities (COX-2: IC50= 0.15 μM, 5-LOX: IC50= 0.85 μM),(ii) 15e selectively inhibited COX-2 relative to COX-1 with selectivity index (SI= 0.012) comparable ...