苯硝唑
硝呋替莫
克鲁兹锥虫
恰加斯病
杀锥虫剂
杀虫药
化学
黄酮类
同色链霉菌
立体化学
生物
生物化学
体外
寄生虫寄主
病毒学
突变体
计算机科学
万维网
基因
色谱法
作者
Luis A González,Sara M. Robledo,Yulieth Upegui,Gustavo Escobar,Winston Quiñones
出处
期刊:Molecules
[Multidisciplinary Digital Publishing Institute]
日期:2021-11-23
卷期号:26 (23): 7067-7067
被引量:4
标识
DOI:10.3390/molecules26237067
摘要
American trypanosomiasis (Chagas disease) caused by the Trypanosoma cruzi parasite, is a severe health problem in different regions of Latin America and is currently reported to be spreading to Europe, North America, Japan, and Australia, due to the migration of populations from South and Central America. At present, there is no vaccine available and chemotherapeutic options are reduced to nifurtimox and benznidazole. Therefore, the discovery of new molecules is urgently needed to initiate the drug development process. Some acetophenones and chalcones, as well as chromane-type substances, such as chromones and flavones, are natural products that have been studied as trypanocides, but the relationships between structure and activity are not yet fully understood. In this work, 26 compounds were synthesized to determine the effect of hydroxyl and isoprenyl substituents on trypanocide activity. One of the compounds showed interesting activity against a resistant strain of T. cruzi, with a half effective concentration of 18.3 µM ± 1.1 and an index of selectivity > 10.9.
科研通智能强力驱动
Strongly Powered by AbleSci AI