Synthesis, Characterization and Evaluation of Anti-inflammatory and Analgesic Activity of Some Novel Quinoline Based Thiazolidinone Heterocycles
作者:Atef Amer、Ali Deeb、Wafaa I. El-Eraky、Sally A. El Awdan、Sebaey Mahgoub
DOI:10.21608/ejchem.2018.5155.1456
日期:2018.12.1
-2-yl)hydrazono)indolin-2-ones 11 and 12, which were converted to 1-substituted 3'-(quinolin-2-ylamino)spiro[indoline-3,2'-thiazolidine]-2,4'-dione 21 and 22 by cyclocondensation with thioglycolic acid. All newly synthesized compounds have been characterized by means of elemental analyses, IR, 1H NMR and MS. Furthermore, all new thiazolidinone derivatives were evaluated for their anti-inflammatory
在本文中,我们报告了三步过程中一些基于喹啉的噻唑烷酮衍生物(13-22)的合成。2-肼基喹啉2与不同的芳族醛缩合得到相应的席夫碱3-10,其随后与巯基乙酸反应以提供相应的噻唑烷酮衍生物13-20。化合物2与伊斯丁或甲基伊斯丁的反应得到1-取代的3-(2-(喹啉-2-基)肼基)吲哚啉-2-酮11和12,它们被转化为1-取代的3'-(喹啉-通过与巯基乙酸的环缩合反应,制得2-基氨基)螺[吲哚啉-3,2'-噻唑烷] -2,4'-二酮21和22。所有新合成的化合物均已通过元素分析,IR,1H NMR和MS进行了表征。此外,评价所有新的噻唑烷酮衍生物的抗炎和镇痛活性。研究结果显示,按照以下22> 17> 13> 14> 21> 15的顺序,通过6种衍生物获得了最高的抗炎药效价,与参考药物消炎痛相比,它具有良好的浮肿抑制作用。与吲哚美辛相比,带有吲哚环系统的化合物22在给药后的第一小时显着抑制了水肿体