Mechanism-based design of simple, symmetrical, easily prepared, potent antimalarial endoperoxides
作者:Gary H. Posner、Dasong Wang、Lluïsa González、Xueliang Tao、Jared N. Cumming、Donna Klinedinst、Theresa A. Shapiro
DOI:10.1016/0040-4039(95)02329-1
日期:1996.2
Mechanism-based design, two-step synthesis, and in vitro antimalarial testing showed thermally stable, crystalline, bicyclic endoperoxides 2a and 2b to be potent antimalarials. Their reduction by FeBr2 proceeds via oxy-radicals and then carbon radicals that undergo β-scission to form an alkene and a high-valent FeO species.
基于机理的设计,两步合成和体外抗疟测试表明,热稳定的结晶双环内过氧化物2a和2b是有效的抗疟药。其通过FeBr还原2个前进通过氧基团,然后碳自由基经历β-断裂以形成烯烃和高价FeO物种。