Literature

Abstract

1-((2,3-Dihydrobenzo[b][1,4]dioxin-6-yl)methyl)-4-substituted-phenylpiperazine moiety was prepared and has been found to be a new and selective ligand for the enzyme cyclooxygenase-2 (COX-2). The biological activity of compound 3k as anti-inflammatory agent was further investigated both in vitro and in vivo. Notably, compound 3k exhibited the best anti-inflammatory activity among the eleven designed compounds with no toxicity, as determined by the ulcerogenic activity. Computational docking studies also showed that compound 3k has interaction with COX-2 key residues in the active site. Compound 3k maybe a new anti-inflammatory lead-candidate as powerful and novel non-ulcerogenic.

DOI： 10.1016/j.bmc.2016.09.023

Synthesis of phenylpiperazine derivatives of 1,4-benzodioxan as selective COX-2 inhibitors and anti-inflammatory agents

Bioorganic & Medicinal Chemistry 2016.0

2-(2-Arylphenyl)benzoxazole As a Novel Anti-Inflammatory Scaffold: Synthesis and Biological Evaluation

ACS Medicinal Chemistry Letters 2014.0

Celecoxib analogs bearing benzofuran moiety as cyclooxygenase-2 inhibitors: Design, synthesis and evaluation as potential anti-inflammatory agents

European Journal of Medicinal Chemistry 2014.0

Synthesis, molecular modeling and anti-inflammatory screening of new 1,2,3-benzotriazinone derivatives

Medicinal Chemistry Research 2012.0

Synthesis, biological evaluation and docking analysis of 3-methyl-1-phenylchromeno[4,3- c ]pyrazol-4(1 H )-ones as potential cyclooxygenase-2 (COX-2) inhibitors

Bioorganic & Medicinal Chemistry Letters 2014.0

Synthesis, cyclooxygenase inhibition, anti-inflammatory evaluation and ulcerogenic liability of new 1,3,5-triarylpyrazoline and 1,5-diarylpyrazole derivatives as selective COX-2 inhibitors