期刊
ACS INFECTIOUS DISEASES
卷 9, 期 5, 页码 1150-1159出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsinfecdis.3c00090
关键词
neolignan-based analogues; BALB; c mice; experimental leishmaniasis; cutaneous leishmaniasis; L; amazonensis; intralesional treatment
This study evaluated the in vivo intralesional treatment efficacy of five isoxazole derivatives and found that analogue 7 showed promising therapeutic effects and low toxicity. It could be a potential new drug candidate for CL caused by L. amazonensis.
New treatment approaches targeting cutaneous leishmaniasis (CL) are required since conventional drugs exhibit limitations due to their several adverse effects and toxicity. In this study, we aimed to evaluate the in vivo intralesional treatment efficacy of five isoxazole derivatives previously synthesized and effective in vitro against intracellular amastigote forms of Leishmania (L.) amazonensis. Among the tested analogues, 7 exhibited relevant in vivo therapeutic effects. The in silico predictions provided interesting information about the toxicity, suggesting the safety of analogue 7. Experiments performed with Salmonella typhimurium strains (TA98, TA100, and TA102) showed a non-mutagenicity profile of 7. The treatment of Leishmania-infected BALB/c mice with isoxazole 7 showed remarkably smaller CL lesions and decreased the parasitism (by 98.4%) compared to the control group. Hence, analogue 7 is a promising drug candidate and alternative treatment for CL caused by L. amazonensis.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据