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New potent 5-nitroindazole derivatives as inhibitors of Trypanosoma cruzi growth: Synthesis, biological evaluation, and mechanism of action studies by Jorge Rodríguez; Vicente J. Arán; Lucía Boiani; Claudio Olea-Azar; María Laura Lavaggi; Mercedes González; Hugo Cerecetto; Juan Diego Maya; Catalina Carrasco-Pozo; Hernán Speisky Cosoy is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

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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.

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Author

Jorge Rodríguez; Vicente J. Arán; Lucía Boiani; Claudio Olea-Azar; María Laura Lavaggi; Mercedes González; Hugo Cerecetto; Juan Diego Maya; Catalina Carrasco-Pozo; Hernán Speisky Cosoy

Publisher

Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0968-0896)

Published

2009

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)