Novel antileishmanial chalconoids: Synthesis and biological activity of 1- or 3-(6-chloro-2H-chromen-3-yl)propen-1-ones

A series of novel chalconoids containing a 6-chloro-2H-chromen-3-yl group were prepared through a convenient and efficient synthetic method by using 5-chloro-2-hydroxybenzaldehyde as starting material. The target compounds were evaluated against the promastigote form of Leishmania major using MTT assay. All of the evaluated compounds have shown high in vitro antileishmanial activity at concentrations less than 3.0 μM. The results of cytotoxicity assessment against mouse peritoneal macrophage cells showed that these compounds display antileishmanial activity at non-cytotoxic concentrations.

Graphical abstractA series of novel chalconoids containing a 6-chloro-2H-chromen-3-yl group were prepared and evaluated against the promastigote form of Leishmania major.Figure optionsDownload full-size imageDownload as PowerPoint slide