In vitro antifungal activity of polyfunctionalized 2-(hetero)arylquinolines prepared through imino Diels–Alder reactions

Diverse polyfunctionalized quinolines, easily prepared using Lewis acid-catalyzed imino Diels–Alder reactions between corresponding aldimines, were tested for antifungal properties against standardized as well as clinical isolates of clinically important fungi. Among them, 4-pyridyl derivatives displayed the best activities mainly against dermatophytes. The activity appears not to be related neither to the lipophilicity nor to the basicity of compounds.

Thirty-three 2-aryl and 2-hetaryl derivatives of polyfunctionalized quinolines (groups 1 and 2) were tested for antifungal properties against standardized and isolates of clinically important fungi. The most active compounds belong to group 2 being playing the positions 4 and 8 of the quinoline ring an important role against dermatophytes.Figure optionsDownload as PowerPoint slide