Novos derivados da nitrofurazona: síntese, toxicidade aguda; estudo das atividades antimicrobiana e antichagásica

by Albuquerque de, Maria Patrícia

Abstract (Summary)
The parasitic infections caused by protozoary affect more than 3 billion people in the worldwide and represent an important pack for economic and health. Despite the persistence in the vaccine development, the chemotherapy it remains the more effectiveisolated way and cheap to control the majority of the microbial and parasitic infections. The nitrofuran derivative, Nitrofurazone (5-nitro-2-furfurilidenosemicarbazone) studied initiallyin the decade of 40, has deserved prominence for dealing with a compound that possess biological activity such as antimicrobials wide-specter of action against Gram-positives and Gram-negative microorganisms, as also powerful action for the acute form of the Chagas? disease. However, this compound presents severe collateral effect and weak liposolubility,requiring great concentrations to get therapeutically effect. In this view, the objective of this work was obtain, by principles of the molecular modification, based on the homologation of the prototype (Nitrofurazone), the attainment and characterization of compound more liposoluble, and consequently, more active and less toxic. The new derivatives of the Nitrofurazone had been prepared by means of the new alkylation way in aprotic solvents, in the position N2 and N2, N4 of the semicarbazone, with good yields and degree of purity. The derivatives N2-monoalkylated had been most active of serie for antimicrobial activity in assay in vitro against several microorganisms, showing more potent than prototype, mainly for Gram-positives strains, including multi-drug resistant S. aureus (MRSA). The antichagasic activity was determined in vitro against epimastigote form of the T. cruzi, Y strain, in which the derivatives N2, N4-dialkylated had been more active than the prototype. The preliminary toxic activity in vivo was carried through for the N2-monobutyl derivative (more potent antimicrobial derivative), with LD50 = 186 mg/kg, showing slightly more toxic than the prototype, however, more liposoluble, facilitating the transport of this drug with larger power of crossing-cell. The gotten results had been good,as much in the developed method and incomes gotten to the new derivatives, as well as the increase of the lipofilia and the potencialization of this, against the microorganisms and to parasite T. cruzi
This document abstract is also available in Portuguese.
Bibliographical Information:

Advisor:Dalci José Brondani

School:Universidade Federal de Pernambuco

School Location:Brazil

Source Type:Master's Thesis

Keywords:derivados da nitrofurazona síntese avaliação toxicidade aguda estudo das atividades antimicrobiana e antichagásica farmacia


Date of Publication:03/15/2006

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