New substituted pyrazole derivatives targeting COXs as potential safe anti-inflammatory agents
| Autor: | Shaimaa G Elzayat, Mohammed T. El-Saadi, Noha H. Amin, Khaled R.A. Abdellatif |
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| Rok vydání: | 2019 |
| Předmět: |
Male
medicine.drug_class Inflammatory response Anti-Inflammatory Agents Pyrazole Pharmacology 01 natural sciences Anti-inflammatory Structure-Activity Relationship chemistry.chemical_compound Catalytic Domain Drug Discovery medicine Animals Edema Rats Wistar Binding Sites biology 010405 organic chemistry business.industry Hydrogen Bonding Rats 0104 chemical sciences Molecular Docking Simulation 010404 medicinal & biomolecular chemistry chemistry Celecoxib Cyclooxygenase 2 Docking (molecular) Cyclooxygenase 1 biology.protein Pyrazoles Molecular Medicine Cyclooxygenase business medicine.drug |
| Zdroj: | Future Medicinal Chemistry. 11:1871-1882 |
| ISSN: | 1756-8927 1756-8919 |
| Popis: | Aim: Everyday studies prove the increasing need for newer and safer agents to control cellular inflammatory response, an underlying cause for the pathophysiology of many other clinical cases. Results: Two newly designed sets of schiff 5a-h and chlacone 6a-f substituted pyrazoles were synthesized and evaluated for their in vivo/vitro anti-inflammatory activities. Most potent representatives were chosen for investigation of ulcerogenic and molecular docking properties. Conclusion: The synthesized compounds showed considerable edema inhibition percentage range if compared with celecoxib (13–93% and 58–93%, respectively) at different time intervals. Compound 6e showed the best screening results if compared with celecoxib (inhibition % = 93.62 and 93.51% at 5 h, COX-1/COX-2 selectivity index SI = 215.44 and 308.16 and ulcer index = 7.25 and 8, respectively). |
| Databáze: | OpenAIRE |
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