Design, Docking, and Synthesis of Some New Pyrazoline and Pyranopyrazole Derivatives as Anti-inflammatory Agents

作者:Ismail Magda M F; Khalifa Nagy M*; Fahmy Hoda H; Nossier Eman S; Abdulla Mohamed M
来源:Journal of Heterocyclic Chemistry, 2014, 51(2): 450-458.
DOI:10.1002/jhet.1757

摘要

Design and synthesis of some novel pyrazoline and pyranopyrazole derivatives as potential anti-inflammatory agents are described. Most of the compounds were tested for their anti-inflammatory (in vitro and in vivo) and ulcerogenic activities. In all tested compounds, it was found that pyrazolines, 2a, and pyrazolopyrano[2,3-d]pyrimidine 9 are the potent anti-inflammatory and selective cyclooxygenase-2 (COX-2) inhibitor. All compounds are mainly in the safe level. Docking study of 2a and 9 revealed higher affinity for binding with the active site of COX-2 enzyme like SC-558, a selective COX-2 inhibitor.

  • 出版日期2014-3