4.4 Article

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

Journal

JOURNAL OF HETEROCYCLIC CHEMISTRY
Volume 51, Issue 2, Pages 450-458

Publisher

WILEY-BLACKWELL
DOI: 10.1002/jhet.1757

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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.

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