Singh Chandan, Malik Heetika, Puri Sunil K
Division of Medicinal and Process Chemistry, Central Drug Research Institute, Lucknow 226001, India.
Bioorg Med Chem Lett. 2005 Oct 15;15(20):4484-7. doi: 10.1016/j.bmcl.2005.07.013.
A new series of functionalized 1,2,4-trioxanes 10-21 have been prepared and assessed for antimalarial activity in mice. Several of these trioxanes show significant activity. Trioxane 16, the most active compound of the series, has shown activity by oral route which is comparable with that of the clinically used drug, beta-arteether.
已制备了一系列新的功能化1,2,4-三氧杂环己烷10 - 21,并在小鼠中评估了其抗疟活性。其中几种三氧杂环己烷显示出显著活性。该系列中活性最强的化合物三氧杂环己烷16经口服给药显示出的活性与临床使用的药物蒿甲醚相当。