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New 5-nitroindazole derivatives were developed and studied as antiproliferative
Trypanosoma cruzi agents.
New 5-nitroindazole derivatives were developed and their antichagasic properties studied. Eight compounds (
14–18,
20,
26 and
28) displayed remarkable in vitro activities against
Trypanosoma cruzi (
T. cruzi). Its unspecific cytotoxicity against macrophages was evaluated being not toxic at a concentration at least twice that of
T. cruzi IC
50, for some derivatives. The electrochemical studies, parasite respiration studies and ESR experiment showed that 5-nitroindazole derivatives not be able to yield a redox cycling with molecular oxygen such as occurs with nifurtimox (Nfx). The study on the mechanism of action proves to be related to the production of reduced species of the nitro moiety similar to that observed with benznidazole.