杜氏利什曼原虫
利什曼病
乙二醇
呋喃妥因
利什曼原虫
体外
化学
药理学
IC50型
微生物学
内脏利什曼病
生物
生物化学
寄生虫寄主
免疫学
抗生素
有机化学
抗生素耐药性
万维网
计算机科学
作者
Keitumetsi Ndlovu,Christina Kannigadu,Janine Aucamp,Helena D. Janse van Rensburg,David D. N’Da
标识
DOI:10.1002/ardp.202200529
摘要
Leishmaniasis is a neglected tropical disease that is caused by the Leishmania parasite. It is estimated that there are more than 350 million people at risk of infection annually. Current treatments that are in clinical use are expensive, have toxic side effects, and are facing parasitic resistance. Therefore, new drugs are urgently required. In the quest for new, safe, and cost-effective drugs, a series of novel ethylene glycol derivatives of nitrofurantoin was synthesised and the in vitro antileishmanial efficacy of the compounds tested against Leishmania donovani and Leishmania major strains. Arylated ethylene glycol derivatives were found to be the most potent, with submicromolar activity up to 294-fold greater than the parent compound nitrofurantoin. Analogues 2j and 2k had the best antipromastigote activities with submicromolar IC50 values against L. major IR-173 and antimonial-resistant L. donovani 9515 strains.
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