AI Article Synopsis
- The study focuses on synthesizing and evaluating 15 new compounds derived from curcuminoids as potential treatments for trypanosomiasis.
- These compounds were created through a cyclization reaction with hydrazines and tested for their effectiveness against trypanosome parasites.
- Two specific derivatives showed significant activity against the parasites while remaining non-toxic to healthy cells, indicating a potential for further development as effective inhibitors.
Article Abstract
We report the synthesis and biological evaluation of a small library of 15 functionalized 3-styryl-2-pyrazolines and pyrazoles, derived from curcuminoids, as trypanosomicidal agents. The compounds were prepared via a cyclization reaction between the corresponding curcuminoids and the appropriate hydrazines. All of the derivatives synthesized were investigated for their trypanosomicidal activities. Compounds and showed significant activity against epimastigotes of , with IC values of 5.0 and 4.2 μM, respectively, accompanied by no toxicity to noncancerous mammalian cells. Compound was found to effectively inhibit triosephosphate isomerase. The up to 16-fold higher potency of these derivatives compared with their curcuminoid precursors makes them a promising new family of inhibitors.
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| http://dx.doi.org/10.4155/fmc-2020-0349 | DOI Listing |
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