Department of Pharmaceutical & Medicinal Chemistry, Royal College of Surgeons in Ireland, Stephens Green, Dublin 2, Ireland.
Bioorg Med Chem Lett. 2011 Oct 15;21(20):6180-3. doi: 10.1016/j.bmcl.2011.07.088. Epub 2011 Jul 29.
A series of phosphoramidate and phosphorothioamidate compounds based on the lead antitubulin herbicidal agents amiprophos methyl (APM) and butamifos were synthesised and evaluated for antimalarial activity. Of these compounds, phosphorothioamidates were more active than their oxo congeners and the nature of both aryl and amido substituents influenced the desired activity. The most active compound was 46, O-ethyl-O-(2-methyl-4-nitrophenyl)-N-cyclopentyl phosphorothioamidate, which was more effective than the lead compound.
一系列基于 lead 抗微管除草剂阿米福司（APM）和丁噻隆的磷酰胺和硫代磷酰胺化合物被合成并评估了它们的抗疟活性。在这些化合物中，硫代磷酰胺比其氧代同系物更具活性，并且芳基和酰胺取代基的性质都影响了所需的活性。最活跃的化合物是 46，O-乙基-O-(2-甲基-4-硝基苯基）-N-环戊基硫代磷酰胺，其比先导化合物更有效。
