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Quinoxaline N,N'-dioxide derivatives and related compounds as growth inhibitors of Trypanosoma cruzi. Structure-activity relationships. 2004
Gabriela Aguirre, and
Hugo Cerecetto, and
Rossanna Di Maio, and
Mercedes González, and
María Elena Montoya Alfaro, and
Andrés Jaso, and
Belén Zarranz, and
Miguel Angel Ortega, and
Ignacio Aldana, and
Antonio Monge-Vega
Departamento de Química Orgánica, Facultad de Química, Facultad de Ciencias, Universidad de la República, Iguá 4225, 11400 Montevideo, Uruguay.
Quinoxaline derivatives presented good inhibitor activity of growth of Trypanosoma cruzi in in vitro assays. The 50% inhibitory doses were of the same order of that of Nifurtimox. Derivative 13, a quinoxaline N,N'-dioxide derivative, and the reduced derivatives 19 and 20 were the most cytotoxic compounds against the protozoan. Structural requirements for optimal activity were studied by computational methods. From statistical analysis we could establish a multiple correlation between activity and lipophilic properties and LUMO energy.
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