Pyrazol(in)e derivatives of curcumin analogs as a new class of anti-<i>Trypanosoma cruzi</i> agents

نویسندگان

چکیده

Aim: We report the synthesis and biological evaluation of a small library 15 functionalized 3-styryl-2-pyrazolines pyrazoles, derived from curcuminoids, as trypanosomicidal agents. Methods &amp; results: The compounds were prepared via cyclization reaction between corresponding curcuminoids appropriate hydrazines. All derivatives synthesized investigated for their activities. Compounds 4a 4e showed significant activity against epimastigotes Trypanosoma cruzi, with IC 50 values 5.0 4.2 ?M, respectively, accompanied by no toxicity to noncancerous mammalian cells. Compound 6b was found effectively inhibit T. cruzi triosephosphate isomerase. Conclusion: up 16-fold higher potency these compared curcuminoid precursors makes them promising new family inhibitors.

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ژورنال

عنوان ژورنال: Future Medicinal Chemistry

سال: 2021

ISSN: ['1756-8919', '1756-8927']

DOI: https://doi.org/10.4155/fmc-2020-0349