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 derivatives

Química Nova

Danniel Delmondes Feitoza²  Antônio José Alves²  José Gildo De Lima²  Janete Magali Araújo¹  Jaciana Santos Aguiar¹  Maria Do Desterro Rodrigues¹  Teresinha Gonçalves Silva¹  Silene Carneiro Do Nascimento¹  Alexandre José Da Silva Góes¹ 

[1] ,Universidade Federal de Pernambuco Departamento de Ciências Farmacêuticas Recife PE ,Brasil

关键词: 4-thiazolidinone;    molecular hybridization;    antimicrobial and cytotoxic activities;   

DOI  :  10.1590/S0100-40422012000400007

来源: SciELO

【 摘 要 】

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.

【 授权许可】

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