In Vivo Antileishmanial Effect of 3,5-Diaryl-isoxazole Analogues Based on Veraguensin, Grandisin, and Machilin G: A Glance at a Preclinical Study.

ACS infectious diseases(2023)

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摘要
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 . Among the tested analogues, exhibited relevant in vivo therapeutic effects. The in silico predictions provided interesting information about the toxicity, suggesting the safety of analogue . Experiments performed with strains (TA98, TA100, and TA102) showed a non-mutagenicity profile of . The treatment of -infected BALB/c mice with isoxazole showed remarkably smaller CL lesions and decreased the parasitism (by 98.4%) compared to the control group. Hence, analogue is a promising drug candidate and alternative treatment for CL caused by .
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关键词
BALB/c mice,L. amazonensis,cutaneous leishmaniasis,experimental leishmaniasis,intralesional treatment,neolignan-based analogues
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