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3-Trifluoromethylquinoxaline N,N'-dioxides as anti-trypanosomatid agents. Identification of optimal anti-T. cruzi agents and mechanism of action studies.

Journal of medicinal chemistry (2011-04-22)
Diego Benitez, Mauricio Cabrera, Paola Hernández, Lucía Boiani, María L Lavaggi, Rossanna Di Maio, Gloria Yaluff, Elva Serna, Susana Torres, María E Ferreira, Ninfa Vera de Bilbao, Enrique Torres, Silvia Pérez-Silanes, Beatriz Solano, Elsa Moreno, Ignacio Aldana, Adela López de Ceráin, Hugo Cerecetto, Mercedes González, Antonio Monge
ABSTRACT

For a fourth approach of quinoxaline N,N'-dioxides as anti-trypanosomatid agents against T. cruzi and Leishmania, we found extremely active derivatives. The present study allows us to state the correct requirements for obtaining optimal in vitro anti-T. cruzi activity. Derivatives possessing electron-withdrawing substituents in the 2-, 3-, 6-, and 7-positions were the most active compounds. With regard to these features and taking into account their mammal cytotoxicity, some trifluoromethylquinoxaline N,N'-dioxides have been proposed as candidates for further clinical studies. Consequently, mutagenicity and in vivo analyses were performed with the most promising derivatives. In addition, with regard to the mechanism of action studies, it was demonstrated that mitochondrial dehydrogenases are involved in the anti-T. cruzi activity of the most active derivatives.

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