New ibuprofen derivatives as H2S and NO donors as safer anti-inflammatory agents
| Autor: | Gehan H. Hegazy, Ghaneya S. Hassan, Noha M. Ibrahim, Samar H. Fahim |
|---|---|
| Rok vydání: | 2019 |
| Předmět: |
Pharmacology
0303 health sciences Gastrointestinal tract Nonsteroidal 010405 organic chemistry medicine.drug_class business.industry Ulcer index Ibuprofen 01 natural sciences Anti-inflammatory 0104 chemical sciences No donors 03 medical and health sciences chemistry.chemical_compound chemistry Edema Drug Discovery medicine Molecular Medicine medicine.symptom business 030304 developmental biology medicine.drug |
| Zdroj: | Future Medicinal Chemistry. 11:3029-3045 |
| ISSN: | 1756-8927 1756-8919 |
| DOI: | 10.4155/fmc-2018-0467 |
| Popis: | Aim: Nonsteroidal anti-inflammatory drugs are expansively used worldwide. However, their prolonged administration is associated with serious side effects, especially gastrointestinal ulceration. Materials & methods: New ibuprofen derivatives hybridized with H2S- or NO-donating moieties were synthesized and evaluated for their anti-inflammatory activity and ulcerogenic effect. COX-1/COX-2 isozymes selectivity test for the most promising derivatives was performed. Molecular docking studies were performed. Results: Most of the compounds showed promising anti-inflammatory activity comparable to that of ibuprofen (% edema inhibition = 76.6 and ulcer index = 21.26) with much better gastrointestinal tract tolerance (ulcer indices ranging from 0 to 14.67), especially compound 2 -H2S donor- (% edema inhibition = 75.5 and ulcer index = 11.75) and compound 16 -NO donor- (% edema inhibition = 65.4 and ulcer index = 8.66). |
| Databáze: | OpenAIRE |
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