Naphthoquinoidal [1,2,3]-triazole, a new structural moiety active against Trypanosoma cruzi

[1,2,3]-Triazole derivatives of nor-β-lapachone were synthesized and assayed against the infective bloodstream trypomastigote form of Trypanosoma cruzi, the etiological agent of Chagas disease. All the derivatives were more active than the original quinones, with IC50/1 day values in the range of 17 to 359 μM, the apolar phenyl substituted triazole 6 being the most active compound. These triazole derivatives of nor-β-lapachone emerge as interesting new lead compounds in drug development for Chagas disease.

Graphical abstractSeveral [1,2,3]-triazole derivatives of nor-β-lapachone were synthesized and found to display potent activity in vitro against Trypanosoma cruzi. These naphthoquinoidal triazoles emerge as interesting new lead compounds in drug development for Chagas disease.Figure optionsDownload full-size imageDownload as PowerPoint slide