Department of Chemistry, Jamia Millia Islamia, Jamia Nagar, New Delhi-110025, India.
Eur J Med Chem. 2010 Apr;45(4):1648-53. doi: 10.1016/j.ejmech.2009.12.051. Epub 2010 Jan 13.
Cyclization of oxime with different aldehydes and ketones under basic condition led to the formation of new dioxazole derivatives and the structure was elucidated by spectral data. The effects of diaoxazoles on the inhibition of growth of Entamoeba histolytica and Giardia intestinalis in vitro have been determined, and selected compounds further investigated for their toxicity. SAR showed that the compounds with 5-nitrothiophene group at the 3-postion of the diaoxazole ring were more active than those with the p-toluene group at the same position. It is interesting to note that the compounds found active against E. histolytica were not found active against G. intestinalis. Toxicity studies showed that the compound 8 and 9 were non-toxic against Vero cell line ATCC CCL-81.
在碱性条件下，肟与不同的醛和酮环化生成新的二噁唑衍生物，并通过光谱数据阐明了其结构。测定了二噁唑对体外抑制溶组织内阿米巴和肠道贾第鞭毛虫生长的影响，并进一步研究了选定的化合物的毒性。构效关系表明，在二噁唑环的 3-位具有 5-硝基噻吩基团的化合物比在同一位置具有对甲苯基团的化合物活性更高。有趣的是，发现对溶组织内阿米巴有效的化合物对肠道贾第鞭毛虫没有活性。毒性研究表明，化合物 8 和 9 对 Vero 细胞系 ATCC CCL-81 无毒性。
