新型双噁唑烷衍生物的合成、表征、抗阿米巴活性和毒性。
Synthesis, characterization, antiamoebic activity and toxicity of novel bisdioxazole derivatives.
机构信息
Department of Chemistry, Jamia Millia Islamia, Jamia Nagar, New Delhi 110025, India.
出版信息
Eur J Med Chem. 2009 Nov;44(11):4747-51. doi: 10.1016/j.ejmech.2009.06.016. Epub 2009 Jun 21.
Cyclization of benzene-1,4-dicarbaldehyde dioxime 1 with different aromatic aldehydes in inert atmosphere yielded the corresponding new bisdioxazoles 2-11. The structure of 2-11 was elucidated by spectral data. In vitro antiamoebic activity was performed against HM1:IMSS strain of Entamoeba histolytica. The results showed that the compounds 3 (IC(50)=1.22 microM), 4 (IC(50)=1.41 microM), 7 (IC(50)=1.05 microM) and 10 (IC(50)=1.01 microM) exhibited better antiamoebic activity than the standard drug metronidazole (IC(50)=1.80 microM). The compounds 3, 4, 7 and 10 were tested for toxicity by MTT assay on H9c2 cardiac myoblasts and the results showed that the compounds 3, 4, 7 and 10 offered remarkable viability of 96.2%, 83.5%, 82% and 89%, respectively at a concentration of 12.5 microg/ml.
1,4-苯二甲醛二肟与不同芳香醛在惰性气氛中环化，得到相应的新双二恶唑啉 2-11。通过光谱数据阐明了 2-11 的结构。对 HM1:IMSS 株溶组织内阿米巴进行体外抗阿米巴活性试验。结果表明，化合物 3（IC（50）=1.22 microM）、4（IC（50）=1.41 microM）、7（IC（50）=1.05 microM）和 10（IC（50）=1.01 microM）的抗阿米巴活性优于标准药物甲硝唑（IC（50）=1.80 microM）。通过 MTT 法在 H9c2 心肌细胞上测试化合物 3、4、7 和 10 的毒性，结果表明化合物 3、4、7 和 10 在 12.5 microg/ml 的浓度下分别提供了 96.2%、83.5%、82%和 89%的显著活力。
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