Synthesis and antiplasmodial evaluation of cyclopropyl analogs of the G-factor bicyclic peroxide
作者:Jérémy Ruiz、Béatrice Tuccio、Robert Lauricella、Marjorie Maynadier、Henri Vial、Christiane André-Barrès
DOI:10.1016/j.tet.2013.05.099
日期:2013.8
New bicyclic peroxyketal comprising cyclopropyl moieties, analogs of the G3-factor, have been synthesized and evaluated against Plasmodium falciparum. They exhibit modest antimalarial activities. In order to investigate their mode of action, Fe(II) induced reduction was managed allowing us to establish mechanisms involved on the basis of the structure of the final products. Self-quenching and polymerization
已经合成了新的包含环丙基部分(G3因子类似物)的双环过氧缩酮,并针对恶性疟原虫进行了评估。他们表现出适度的抗疟疾活动。为了研究它们的作用方式,对Fe(II)诱导的还原进行了管理,从而使我们能够根据最终产物的结构建立参与的机制。自猝灭和聚合似乎是主要的降解方式。