Department of Pharmacology, Medical Division, National Research Centre, 33 EL Bohouth st. (former EL Tahrir st.), Dokki, Giza P.O. 12622, Egypt.
Department of Chemistry, Faculty of Science, Cairo University, Giza 12613, Egypt.
Mini Rev Med Chem. 2018;18(16):1409-1421. doi: 10.2174/1389557518666180330101447.
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.
we interested herein to prepare new anti-inflammatory and analgesic agents analogues to Indomethacin in short reaction time by using microwaves irradiation.
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.
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.
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.
微波辅助反应相对于传统方法反应具有显著的优势，因为前者可以在广泛的有机反应中实现显著的速率提高。
我们有兴趣在短时间内通过微波辐射来制备新的具有抗炎和镇痛作用的吲哚啉类似物。
通过将酰肼氯或卤代活性亚甲基衍生物与缩氨基硫脲衍生物反应，在微波辐射下合成了具有噻唑部分的新型腙吲哚啉。此外，还证明了多功能吲哚啉-2,3-二酮衍生物在设计新的多功能砌块方面的用途，可通过与肼衍生物缩合来实现。
所有产物均在短时间内和高收率下形成。形成化合物的光谱数据提供的信息证实了它们的结构。此外，还对设计的衍生物进行了镇痛和抗炎活性筛选，结果表明，六个衍生物 4g、9b、4c、10b、4d 和 11a 表现出最高的抗炎和镇痛作用。
在这方面，我们成功地设计并合成了新的抗炎和镇痛吲哚啉类似物，反应时间短，产率高。
