Indomethacin Analogs: Synthesis, Anti-inflammatory and Analgesic Activities of Indoline Derivatives.

Autor:	Amin MM; Department of Pharmacology, Medical Division, National Research Centre, 33 EL Bohouth st. (former EL Tahrir st.), Dokki, Giza P.O. 12622, Egypt., Shaaban MR; Department of Chemistry, Faculty of Science, Cairo University, Giza 12613, Egypt.; Department of Chemistry, Faculty of Applied Science, Umm Al-Qura University, Makkah Almukkarramah, Saudi Arabia., Al-Qurashi NT; Department of Chemistry, Faculty of Applied Science, Umm Al-Qura University, Makkah Almukkarramah, Saudi Arabia., Mahmoud HK; Department of Chemistry, Faculty of Science, Cairo University, Giza 12613, Egypt., Farghaly TA; Department of Chemistry, Faculty of Science, Cairo University, Giza 12613, Egypt.; Department of Chemistry, Faculty of Applied Science, Umm Al-Qura University, Makkah Almukkarramah, Saudi Arabia.
Jazyk:	angličtina
Zdroj:	Mini reviews in medicinal chemistry [Mini Rev Med Chem] 2018; Vol. 18 (16), pp. 1409-1421.
DOI:	10.2174/1389557518666180330101447
Abstrakt:	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. (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.)
Databáze:	MEDLINE
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