Design, synthesis and application of quinolinone fumaramide derivatives

• Main Authors: LI BAIHUI, JI QINGGANG
• Format: Patent
• Language: Chinese; English
• Published: 21.01.2020
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The invention discloses design, synthesis and application of an N1-(2-oxo-1,2,3,4-tetrahydroquinoline-3-yl)-N4-phenyl fumamide compound. The structure of the compound is shown as a general formula I,wherein R is hydrogen, methyl, ethyl, methoxyl and the like. Bioactivity test experiments prove that the compound has obvious inhibitory activity on chitin synthase, has good inhibitory activity on fungi such as candida albicans, aspergillus flavus, cryptococcus neoformans and aspergillus fumigatus, and can be used for preparing antifungal drugs. 本文公开了N-（2-氧代-1,2,3,4-四氢喹啉-3-基）-N-苯基富马酰胺类化合物的设计合成及应用，所述化合物的结构如通式Ι所示：式中R为氢，甲基，乙基，甲氧基等。经生物活性测试实验证明，化合物对几丁质合成酶抑制活性明显，对白色念珠菌、黄曲霉菌、新型隐球菌和烟曲霉菌等真菌表现出较好的抑制活性，可用于制备抗真菌的药物。