Synthesis and biological characterization of new aryloxyindole-4,9-diones as potent trypanosomicidal agents
Ricardo A Tapia1, Cristian O Salas1, Karina Vázquez1
1Departamento de Química Orgánica, Facultad de Química, Pontificia Universidad Católica de Chile, Santiago 6094411, Chile.
Abstract:
A new indole-4,9-dione and their phenoxy derivatives were synthesized and evaluated in vitro against the epimastigote form of Trypanosoma cruzi, Y strain. All of these novel compounds were found to be extremely potent and selective that the standard drug nifurtimox. Interestingly, phenoxyindole-4,9-dione 9d displayed excellent nanomolar inhibitory activity, IC50=20 nM, and high selectivity index, SI=625. In silico studies using MOE program were performed to generate a preliminary pharmacophore model.
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