
handle: 11449/70774
Durante o planejamento estrutural de novos fármacos, é possível prever a infl uência de grupamentos específi cos na atividade farmacológica. Entre estes, encontrase o grupo nitro, que possui potencial atividade antimicrobiana, estando presente em diversos fármacos como o metronidazol, nitrofural, furazolidona, oxamniquina, cloranfenicol, entre outros. Também, a introdução do grupo nitro na molécula pode alterar as propriedades físico-químicas e eletrônicas da substância, estando presente em fármacos de outras classes terapêuticas como anti-úlcera, ansiolítico, antiinfl amatório. Entretanto, restrições têm sido apontadas para o planejamento de novos fármacos contendo este grupo, devido à toxicidade relacionada. Este estudo trata-se da revisão sobre a toxicidade de compostos nitrofurânicos, bem como os possíveis mecanismos e a utilização do método de latenciação na diminuição desta toxicidade.
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.
Salmonella typhimurium, chloramphenicol, trypanosomiasis, toxicidade, nitrofurantoin, nifurtimox, drug carcinogenicity, metronidazole, ranitidine, antibacterial activity, Prodrug, Pharmaceutical industry, benznidazole, drug effect, oxamniquine, quantitative structure activity relation, nitrofuranos, molecular mechanics, nifurtoinol, chromosome breakage, Nitrofuran, Mechanism, HD9665-9675, chemical modification, primaquine, drug design, review, nitrofural, secnidazole, nimesulide, Pharmacy and materia medica, nitrofuranos; toxicidade; mecanismos; pró-fármacos, chemical composition, micronucleus, human, clonazepam, furazolidone, tinidazole, leishmaniasis, nonhuman, Toxicity, genotoxicity, LD 50, bacterial infection, mutagenicity, RS1-441, drug structure, cell proliferation, DNA damage, mecanismos, nitrofuran derivative
Salmonella typhimurium, chloramphenicol, trypanosomiasis, toxicidade, nitrofurantoin, nifurtimox, drug carcinogenicity, metronidazole, ranitidine, antibacterial activity, Prodrug, Pharmaceutical industry, benznidazole, drug effect, oxamniquine, quantitative structure activity relation, nitrofuranos, molecular mechanics, nifurtoinol, chromosome breakage, Nitrofuran, Mechanism, HD9665-9675, chemical modification, primaquine, drug design, review, nitrofural, secnidazole, nimesulide, Pharmacy and materia medica, nitrofuranos; toxicidade; mecanismos; pró-fármacos, chemical composition, micronucleus, human, clonazepam, furazolidone, tinidazole, leishmaniasis, nonhuman, Toxicity, genotoxicity, LD 50, bacterial infection, mutagenicity, RS1-441, drug structure, cell proliferation, DNA damage, mecanismos, nitrofuran derivative
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