Antimalarial activity of N-alkyl amine, carboxamide, sulfonamide, and urea derivatives of a dispiro-1,2,4-trioxolane piperidine
Antimalarial activity of N-alkyl amine, carboxamide, sulfonamide, and urea derivatives of a dispiro-1,2,4-trioxolane piperidine
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DOI：
10.1016/j.bmcl.2006.08.046
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发表时间：
2006-11-01
影响因子：
2.7
通讯作者：
Vennerstrom, Jonathan L.
中科院分区：
文献类型：
--
作者：
Padmanilayam, Maniyan;Scorneaux, Bernard;Vennerstrom, Jonathan L.
为了鉴定具有高口服活性和良好理化性质的二螺-1,2,4-三氧戊环，合成了27种非手性哌啶三氧戊环衍生物；大多数是有效的抗疟过氧化物，IC(50) 范围为 0.20 至 7.0 ng/mL。其中两种药物的口服疗效优于青蒿琥酯，与蒿甲醚相当。这些化合物具有吸引力的化学简单性仅通过明显的代谢敏感性来平衡。 (c) 2006 Elsevier Ltd. 保留所有权利。
With an aim to identify a dispiro-1,2,4-trioxolane with high oral activity and good physicochemical properties, 27 derivatives of an achiral piperidine trioxolane were synthesized; most were potent antimalarial peroxides with IC(50)s ranging from 0.20 to 7.0 ng/mL. The oral efficacies of two of these were superior to artesunate and comparable to artemether. The attractive chemical simplicity of these compounds is balanced only by an apparent metabolic susceptibility. (c) 2006 Elsevier Ltd. All rights reserved.