Synthesis of novel 6-substituted-3-formyl chromone derivatives as anti-leishmanial agents and their possible mechanism of action in Leishmania donovani
2023; Elsevier BV; Volume: 1280; Linguagem: Inglês
10.1016/j.molstruc.2023.135081
ISSN1872-8014
AutoresElier Galarraga, Angel Santorelli, Neudo Urdaneta, André Rey-Cibati, Mariana Valladares-Delgado, Luis José Díaz-Pérez, Laura Milano-Franco, Gustavo Benaím,
Tópico(s)Synthesis and Reactivity of Sulfur-Containing Compounds
ResumoEleven new compounds, including the hydrazones 4a-h, pyrazole 5, and pyrazole-oximes 7b-c, were synthesized by condensation reaction between 6-substituted (-H, -Me, -F) 3-formylchromones 1a-c with N-substituted hydrazines 2a-d and hydroxylamine hydrochloride 3. The synthesized compounds were evaluated for their in vitro antileishmanial activity to determine the IC50 values. Compounds 4b, 4c and 4e exhibited the strongest antileishmanial activity with IC50 values between 1.6 – 4.7 µm. A plausible mechanism of action is proposed for the antileishmanial activity of the above-mentioned compounds. We also studied the effect of these three compounds on macrophages, which represent the mammalian host-cell. The results obtained on this system were about one order of magnitude larger when compared to those of L. donovani, thus supporting these compounds potential as precursors of antileishmanial drugs.
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