| 李刚,李倩,蒋璐毅,王鸣旭,李卫,祁艳艳,李干鹏.化学通报,2024,87(7):857-863,844. |
| 含吲哚啉酮取代基的噻唑酮类化合物的合成及其抗菌活性研究 |
| Synthesis and Antibacterial Activity of Thiazolidones Containing Indolinone Substituents |
| 投稿时间：2024-01-03 修订日期：2024-01-19 |
| DOI： |
| 中文关键词: 噻唑酮 吲哚酮 抗菌活性 白念珠菌 |
| 英文关键词:Thiazolone Indolone Antimicrobial activity Candida albicans |
| 基金项目:云南省创新团队项目(2019HC020)资助 |
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| 摘要点击次数: 418 |
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| 中文摘要: |
| 目的：合成一系列含吲哚啉酮骨架的噻唑酮类化合物并对其进行抗耐药白念珠菌活性筛选。方法：以不同取代基的4-苯基噻唑-2(3H)-酮和不同取代的2-苯基-3H-吲哚-3-酮为起始原料,进行Friedel-Crafts烷基化反应,优化并合成一系列目标衍生物,并采用微量稀释法对合成的化合物进行了抗真菌活性研究。结果与讨论：报道了一种新型合成含吲哚啉酮取代基的噻唑酮类化合物的方法,优化反应条件后以良好至优秀的产率得到了22个化合物。微量稀释法测试结果显示,合成的化合物其效果除了化合物17,18效果较差以外,其余20个化合物效果优秀,值得进一步探讨和研究。 |
| 英文摘要: |
| Objective: To synthesize a series of thiazolidones containing indolinone backbone and screen their activities against drug-resistant Candida albicans. Methods: 4-phenylthiazol-2 (3H) -one with different substituents and 2-phenyl-3H-indole-3-one were used as starting materials to perform Friedel-Crafts alkylation reaction. A series of target derivatives were optimized and synthesized, and their antifungal activities were studied by microdilution method. Results and DISCUSSION: A new method for the synthesis of thiazolidones containing indolinone substituents was reported. After optimizing the reaction conditions, 22 compounds were obtained in good to excellent yields. The results of microdilution test showed that compounds 17 and 18 had poor effects, while the other 20 compounds had excellent effects, which were worthy of further exploration and research. |
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