Design,Docking, and Synthesis of Some New Pyrazoline and Pyranopyrazole Derivatives as Anti‐inflammatory Agents |
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| Authors: | Magda M F Ismail Nagy M Khalifa Hoda H Fahmy Eman S Nossier Mohamed M Abdulla |
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| Institution: | 1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy (Girls), Al‐Azhar University, Cairo, Egypt;2. Drug Exploration and Development Chair (DEDC), College of Pharmacy, King Saud University, Riyadh, Saudi Arabia;3. Department of Theraputical Chemistry, Pharmaceutical and Drug Industries Division, National Research Centre, Giza, Egypt;4. Research Unit, Saco Pharm. Co., 6th October City, Egypt |
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| Abstract: | 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 pyrazolopyrano2,3‐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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