|
Química Nova 2012
Synthesis, antimicrobial and cytotoxic activities of 5-benzylidene-2-[(pyridine-4-ylmethylene)hydrazono]-thiazolidin-4-one and 2-[(pyridine-4-ylmethylene) hydrazono]-thiazolidin-4-one derivativesDOI: 10.1590/S0100-40422012000400007 Keywords: 4-thiazolidinone, molecular hybridization, antimicrobial and cytotoxic activities. Abstract: a new series of 5-benzylidene-2-[(pyridine-4-ylmethylene)hydrazono]-thiazolidin-4-ones 4a-l have been synthesized. these compounds were designed by a molecular hybridization approach. 2-[(pyridine-4-ylmethylene)hydrazono]-thiazolidin-4-ones 3a-d were also obtained and used as intermediates to give the target compounds. the in vitro antimicrobial and cytotoxic activities were evaluated for both series. the intermediate 3b showed considerable antibiotic activity against b. subtilis and c. albicans. in the cytotoxic activity compounds 3b (ic50= 4.25 ± 0.36 μg/ml) and 4l (ic50= 1.38 ± 0.04 μg/ml) were effective for inhibition of human erythromyeloblastoid leukemia (k-562) and human lung carcinoma (nci-h292) cell lines, respectively.
|