Estudo químico e biológico de derivados da Tiazolidina-2,4-diona e 4-Tioxo-tiazolidina-2-ona

by Silva Filho, João da

Abstract (Summary)
Thiazolidines are five membred heterocycle compounds ring containing oxygen and sulfur in their structure. They show microbiological and pharmacological properties as hypoglycemic, analgesic, anti-inflammatory, etc. This work seeks to synthesize new thiazolidinics derivatives characterized by the substitution of the positions 3, 4 and 5 of the thiazolidine-2,4-dione by different radicals observing their biological activity. The derivatives were prepared by reactions of N-alkylation with 6-chloroacetyl-1,4-benzoxazin-3-one (benzoxazone) refluxing in methanol/KOH and condensation with substituted aromatic aldehydes, using pyridine and methanol or sodium acetate and acetic acid. The compounds obtained were submitted to biological assays for determination of the anti-microbiological, cytotoxic and anti-oxidant activities. The antimicrobial activity was evaluated qualitative, by disk diffusion method and quantitatively by determination of the minimum inhibition concentration (MIC) and minimum bactericidal concentration (MBC), against 10 pathogen microorganisms, including Gram-positive bacteria, Gram-negative, bacilli alcohol-acid resistant, yeasts and filamentous mushrooms. The cytotoxic activity was accomplished with lineage cells HEp-2 (Cancer Epidermoid of Larynx) and lineages NCI-H292 (Lung). For the antioxidantactivity 0,1 mL was used (3,7 MBq) of Tc-99m in the sodium pertecnetate (99m TcO4Na) form. To evaluate the connection potential in the cells of the blood and plasma of mouse wistar. Six new compounds were obtained and their chemical structures were established by spectroscopic methods. All the compounds were submitted to qualitative microbiological evaluation, that of larger inhibition was submitted the determination of MIC. The compounds presented cytotoxic inhibition varying from 30 to 80% to the two lineages. One derived it presented low anti-oxidant action
This document abstract is also available in Portuguese.
Bibliographical Information:

Advisor:Julianna Ferreira Cavalcanti de Albuquerque

School:Universidade Federal de Pernambuco

School Location:Brazil

Source Type:Master's Thesis

Keywords:compostos heterocíclicos aromáticos tiazolidina 2 4 diona e tioxo ona quimica dos produtos naturais síntese de derivados tiazolidínico estudo químico biológico


Date of Publication:02/26/2004

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