Singh Chandan, Malik Heetika, Puri Sunil K
Division of Medicinal Chemistry, Central Drug Research Institute, -226001, Lucknow, India.
Bioorg Med Chem Lett. 2004 Jan 19;14(2):459-62. doi: 10.1016/j.bmcl.2003.10.051.
Using readily available trioxanes 6a-b, a new series of amino functionalized 1,2,4-trioxanes 8a-e and 9a-e have been prepared and evaluated for antimalarial activity against multi-drug resistant Plasmodium yoelii in Swiss mice model. Several of these novel trioxanes are orally more active than the parent trioxanes 6a-b. Antimalarial activity of amino functionalized trioxane 9a, the most potent compound in the series, is very close to that of beta-arteether.
利用易于获得的三恶烷6a - b，制备了一系列新的氨基官能化1,2,4 - 三恶烷8a - e和9a - e，并在瑞士小鼠模型中针对多药耐药的约氏疟原虫进行了抗疟活性评估。这些新型三恶烷中有几种口服活性比母体三恶烷6a - b更高。该系列中最有效的化合物——氨基官能化三恶烷9a的抗疟活性与蒿甲醚非常接近。
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