2. Academic Validation
  3. Synthesis, antimicrobial and cytotoxic activities of some 5-arylidene-4-thioxo-thiazolidine-2-ones

Synthesis, antimicrobial and cytotoxic activities of some 5-arylidene-4-thioxo-thiazolidine-2-ones

  • Eur J Med Chem. 2009 May;44(5):2038-43. doi: 10.1016/j.ejmech.2008.10.006.
Frederico L Gouveia 1,  Renata M B de Oliveira,  Tatiane B de Oliveira,  Ivanildo M da Silva,  Silene C do Nascimento,  Kêsia X F R de Sena,  Julianna F C de Albuquerque
Affiliations

Affiliation

  • 1 Departamento de Ciências Farmacêuticas, Universidade Federal de Pernambuco, Recife 50670-901, Brazil.
PMID: 19027993 DOI: 10.1016/j.ejmech.2008.10.006
Abstract

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.

Figures