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Matiadis, Dimitris; Saporiti, Tatiana; Aguilera, Elena; Robert, Xavier; Guillon, Christophe; Cabrera, Nallely; Perez-Montfort, Ruy; Sagnou, Marina; Alvarez, Guzman (2021)

PYRAZOL(IN)E DERIVATIVES OF CURCUMIN ANALOGS AS A NEW CLASS OF ANTI-TRYPANOSOMA CRUZI AGENTS

Future Med Chem ():
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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.