Dillapiole as Antileishmanial Agent: Discovery, Cytotoxic Activity and Preliminary SAR Studies of Dillapiole Analogues

In this paper, the isolation of dillapiole (1)fromPiperaduncumwas reported as well as the semi-synthesisof two phenylpropanoid derivatives [di-hydrodillapiole (2), isodillapiole (3)], via reduction andisomerization reactions. Also, the compounds’ molecular properties (structural, electronic,hydrophobic, and steric) were calculated and investigated to establish some preliminary structure–activity relationships (SAR). Compounds were evaluated for in vitro antileishmanial activity andcytotoxic effects on fibroblast cells. Compound 1 presented inhibitory activity against Leishmaniaamazonensis (IC