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Eur J Med Chem ; 44(5): 2038-43, 2009 May.
Artigo em Inglês | MEDLINE | ID: mdl-19027993

RESUMO

Several 5-arylidene-4-thioxo-thiazolidine-2-ones (3a-n) were synthesized and evaluated as antimicrobial agents against representative strains, including multidrug-resistant strains of clinical isolates. Also, the antiproliferative activity was evaluated against two human carcinoma cell lines (NCI-H292 and HEp-2). The compounds containing the 5-arylidene subunit presented greater antimicrobial activities against Gram positive bacteria, including the multidrug-resistant clinical isolates, than the 4-thioxo-thiazolidine-2-one. Important SAR information was also gathered, such as the contribution of thiocarbonyl attached at 4-position on the thiazolidine heterocyclic for antimicrobial properties. None of the derivatives exhibited significant antiproliferative activity against the human carcinoma cell lines.


Assuntos
Anti-Infecciosos/síntese química , Tiazolidinas/síntese química , Anti-Infecciosos/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Resistência a Múltiplos Medicamentos , Ensaios de Seleção de Medicamentos Antitumorais , Bactérias Gram-Positivas/efeitos dos fármacos , Humanos , Cetonas , Testes de Sensibilidade Microbiana , Relação Estrutura-Atividade , Tiazolidinas/farmacologia
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