AI Article Synopsis
- Cutaneous leishmaniasis (CL) is a neglected tropical disease that causes severe skin lesions, and there is a pressing need for new treatment options due to the limitations of current drugs and vaccines.
- Researchers synthesized 18 acyl hydrazone derivatives of thiochroman-4-ones and tested their effectiveness against the intracellular form of the parasite and their toxicity to human monocytes.
- The study found that certain derivatives significantly improved antileishmanial activity, particularly semicarbazone and thiosemicarbazone derivatives, which exhibited high effectiveness with low toxicity, indicating promising selectivity for future treatments.
Article Abstract
Cutaneous leishmaniasis (CL) is a neglected tropical disease, which causes severe skin lesions. Due to the lack of effective vaccines, and toxicity or reduced effectiveness of available drugs in addition to complex and prolonged treatments, there is an urgent need to develop alternatives for the treatment for CL with different mechanisms of action. In our effort to search for new promising hits against parasites we prepared 18 acyl hydrazone derivatives of thiochroman-4-ones. Compounds were evaluated for their in vitro antileishmanial activity against the intracellular amastigote form of and cytotoxic activity against human monocytes (U-937 ATCC CRL-1593.2). Our results show that derivatization of the thiochroman-4-ones with acyl hydrazones significantly enhances the antileishmanial activity. Among the compounds tested semicarbazone and thiosemicarbazone derivatives of thioflavanone and displayed the highest antileishmanial activities, with EC values of 5.4 and 5.1 µM and low cytotoxicities (100.2 and 50.1 µM respectively), resulting in higher indexes of selectivity (IS).
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6017792 | PMC |
| http://dx.doi.org/10.3390/molecules23010070 | DOI Listing |
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