Abstract

Pyridine acylhydrazone derivatives of isopimaric acid were synthesized and characterized. The minimum inhibitory concentrations of the compounds against five bacteria were determined and most of the compounds displayed some degree of antibacterial activity. The results showed that antimicrobial activity against Streptococcus pneumoniae improved when halogen atoms were introduced into the isopimaric acid, especially when one bromine atom was introduced in the para-position of isopimaric acid. Compound isopimaric acid (5-bromo pyridine-2-formaldehyde) acylhydrazone exhibited a significant antitumorial activity against hepatocarcioma cells (HepG-2) and breast cancer cells (MDA-MB-231), with inhibition degrees of 74.21% and 70.39%, respectively, at 100 μM.

摘要

合成并表征了异海松酸的吡啶酰基hydr衍生物。确定了化合物对五种细菌的最低抑制浓度，大多数化合物表现出一定程度的抗菌活性。结果表明，当将卤素原子引入异海藻酸中时，尤其是当将一个溴原子引入异海藻酸的对位时，对肺炎链球菌的抗菌活性得到改善。化合物异海藻酸（5-溴吡啶-2-甲醛）酰基hydr对肝癌细胞（HepG-2）和乳腺癌细胞（MDA-MB-231）表现出显着的抗肿瘤活性，抑制率分别为74.21％和70.39％。 ，浓度为100μM。