Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow, India.
Bioorg Med Chem Lett. 2012 Feb 15;22(4):1527-32. doi: 10.1016/j.bmcl.2012.01.009. Epub 2012 Jan 10.
A series of 3,6-epoxy [1,5]dioxocines were synthesized and evaluated for their antifilarial activity against adult parasites of human lymphatic filarial parasite Brugia malayi (sub-periodic strain) in vitro. Out of these, six compounds (4a-f) possessed improved in vitro anti-filarial activity and examples 4d and 4f were also found to be active in the in vivo experiments. These results demonstrate that 3,6-epoxy [1,5]dioxocines exhibits potent antifilarial activity and might be developed into a new class of antifilarial drug.
一系列 3,6-环氧[1,5]二氧杂环辛烷被合成并评估其对体外人体淋巴丝虫寄生虫布鲁氏线虫（亚周期性株）成虫的抗丝虫活性。在这些化合物中，有 6 种（4a-f）具有改善的体外抗丝虫活性，并且还发现化合物 4d 和 4f 在体内实验中也具有活性。这些结果表明 3,6-环氧[1,5]二氧杂环辛烷具有很强的抗丝虫活性，可能被开发成一类新的抗丝虫药物。
