Microwave-assisted synthesis and pharmacological screening of some triazolothiadiazole derivatives
| Autor: | Kevser Erol, Yeşim Özkan, Tijen Önkol, Bilge Çakir, Engin Yildirim, Ozge Gorgu |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2020 |
| Předmět: |
Chemistry
Antinociceptive activity 2(3H)-Benzoxazolone 030226 pharmacology & pharmacy 01 natural sciences Microwave assisted 0104 chemical sciences Microwave-assisted synthesis RS1-441 010404 medicinal & biomolecular chemistry 03 medical and health sciences 0302 clinical medicine Pharmacy and materia medica Thiadiazoles Elemental analysis Microwave irradiation Triazolothiadiazole Hot plate Reference standards Nuclear chemistry |
| Zdroj: | Brazilian Journal of Pharmaceutical Sciences, Vol 56 (2020) Brazilian Journal of Pharmaceutical Sciences, Volume: 56, Article number: e18111, Published: 16 MAR 2020 Brazilian Journal of Pharmaceutical Sciences; Vol. 56 (2020); e18111 Brazilian Journal of Pharmaceutical Sciences; v. 56 (2020); e18111 Brazilian Journal of Pharmaceutical Sciences Universidade de São Paulo (USP) instacron:USP |
| ISSN: | 2175-9790 1984-8250 |
| Popis: | In this study, twenty-two new [1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles (5a-n, 6a-h) were synthesized under microwave irradiation (MWI). The chemical structures of the compounds were elucidated by their IR, 1 H-NMR, LC-MS, and elemental analysis. The compounds were tested for antinociceptive activity by using the tail clip, tail flick, hot plate, and writhing methods in mice. The varying levels of antinociceptive activity of the compounds were compared with those of aspirin. Among these compounds, compound 5g and 5j were found to be significantly more active than the other compounds and the standard in the tests. Also, inhibitory effects of the test compounds on COX-1 and COX-2 activities were investigated. DuP-697 for COX-2 and SC-560 for COX-1 were used as reference standards. |
| Databáze: | OpenAIRE |
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