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Merck

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

European journal of medicinal chemistry (2007-11-30)
Eufrânio N da Silva, Rubem F S Menna-Barreto, Maria do Carmo F R Pinto, Raphael S F Silva, Daniel V Teixeira, Maria Cecília B V de Souza, Carlos Alberto De Simone, Solange L De Castro, Vitor F Ferreira, Antônio V Pinto
ZUSAMMENFASSUNG

[1,2,3]-Triazole derivatives of nor-beta-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 IC(50)/1 day values in the range of 17 to 359 microM, the apolar phenyl substituted triazole 6 being the most active compound. These triazole derivatives of nor-beta-lapachone emerge as interesting new lead compounds in drug development for Chagas disease.

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