Singh Chandan, Pandey Shilpi, Kushwaha Ambuj K, Puri Sunil K
Division of Medicinal & Process Chemistry, Central Drug Research Institute, Lucknow 226001, India.
Bioorg Med Chem Lett. 2008 Oct 1;18(19):5190-3. doi: 10.1016/j.bmcl.2008.08.096. Epub 2008 Aug 29.
A series of new amino functionalized 1,2,4-trioxepanes 8-16 and ester functionalized 1,2,4-trioxepanes 17-19 have been synthesized and evaluated against multi-drug resistant Plasmodium yoelii in Swiss mice. Amino functionalized trioxepanes 14, the most active compound of the series, showed 100% clearance of parasitaemia by oral route on day 4 and 75% protection to the treated mice beyond day 28.
一系列新的氨基官能化1,2,4 - 三氧杂环庚烷8 - 16和酯官能化1,2,4 - 三氧杂环庚烷17 - 19已被合成,并在瑞士小鼠中针对多药耐药的约氏疟原虫进行了评估。该系列中最具活性的化合物氨基官能化三氧杂环庚烷14,经口服给药后在第4天实现了100%的血原虫清除率,并且在第28天之后对受试小鼠提供了75%的保护作用。