Toxicidade de fármacos nitrofurânicos

• Autor(a) principal: Bosquesi, P. L. [UNESP]
• Data de Publicação: 2008
• Outros Autores: Almeida, Adelia Emilia de [UNESP], Blau, L. [UNESP], Menegon, R. F. [UNESP], Santos, Jean Leandro dos [UNESP], Chin, Chung Man [UNESP]
• Tipo de documento: Artigo
• Idioma: por
• Título da fonte: Repositório Institucional da UNESP
• Texto Completo: http://serv-bib.fcfar.unesp.br/seer/index.php/Cien_Farm/article/view/588; http://hdl.handle.net/11449/70774
• topic: Mechanism; Nitrofuran; Prodrug; Toxicity; benznidazole; chloramphenicol; clonazepam; furazolidone; metronidazole; nifurtimox; nifurtoinol; nimesulide; nitrofural; nitrofuran derivative; nitrofurantoin; oxamniquine; primaquine; ranitidine; secnidazole; tinidazole; antibacterial activity; bacterial infection; cell proliferation; chemical composition; chemical modification; chromosome breakage; DNA damage; drug carcinogenicity; drug design; drug effect; drug structure; genotoxicity; human; LD 50; leishmaniasis; micronucleus; molecular mechanics; mutagenicity; nonhuman; quantitative structure activity relation; review; Salmonella typhimurium; trypanosomiasis

During the structural designing of new drugs, it is possible predict the influence of specific chemical groups on pharmacological activity. Among these, the nitro group has potential antiparasitic activity, being present in many antimicrobial drugs, such as metronidazole, nitrofurazone, furazolidone, oxamniquine and chloramphenicol. Also, the introduction of the nitro group into a molecule can modify the physicochemical and electronic properties of the substance. Besides antimicrobial drugs, this group is also found in other drug classes, such as antiulcer, anti-inflamatory and anxiolytic. However, the use of the nitro group in drug design has encountered restrictions, due to the associated toxicity. This article is a review of the toxicity of nitrofuran compounds, as well the possible mechanisms involved and the strategy of latentiation by molecular modification to decrease their toxicity.