Indomethacin Analogs: Synthesis, Anti-inflammatory and Analgesic Activities of Indoline Derivatives
| Autor: | Huda K. Mahmoud, Thoraya A. Farghaly, Mohamed R. Shaaban, Mohamed M. Amin, Nadia T. Al-Qurashi |
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| Rok vydání: | 2018 |
| Předmět: |
Male
Indoles Indomethacin Drug Evaluation Preclinical Context (language use) 010402 general chemistry 01 natural sciences Rats Sprague-Dawley Mice Structure-Activity Relationship chemistry.chemical_compound Drug Discovery Animals Moiety Methylene Thiazole Semicarbazone Pharmacology Analgesics 010405 organic chemistry Chemistry Anti-Inflammatory Agents Non-Steroidal General Medicine Combinatorial chemistry 0104 chemical sciences Molecular Docking Simulation Organic reaction Yield (chemistry) Indoline |
| Zdroj: | Mini-Reviews in Medicinal Chemistry. 18:1409-1421 |
| ISSN: | 1389-5575 |
| DOI: | 10.2174/1389557518666180330101447 |
| Popis: | Background Microwave assisted reactions offer a considerable advantages over conventional method reactions because the former results in substantial rate enhancement in a wide range of organic reactions. Objective we interested herein to prepare new anti-inflammatory and analgesic agents analogues to Indomethacin in short reaction time by using microwaves irradiation. Method Synthesis of new hydrazonoindolines having thiazole moiety under microwave irradiation were achieved via the reaction of hydrazonoyl chlorides or halogenated active methylene derivatives with thiosemicarbazone derivatives. Also, the utility of the versatile indoline-2,3-dione derivatives in the design of new multifunctional building blocks using condensation with hydrazine derivatives was demonstrated. Results All products were formed in short reaction time and high yield. The information derived from the spectral data of the formed compounds was confirmed their structures. Also, the analgesic and antiinflammatory activities of the designed derivatives were screened and the results obtained indicated that six derivatives 4g, 9b, 4c, 10b, 4d and 11a revealed the highest anti-inflammatory and analgesic effects. Conclusion we succeeded in this context to design and synthesis of new anti-inflammatory and analgesic agents analogues to Indomethacin in short reaction time and with high yield. |
| Databáze: | OpenAIRE |
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