Weak base dispiro-1,2,4-trioxolanes: Potent antimalarial ozonides
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- 作者：Yuanqing Tang ; Yuxiang Dong ; Sergio Wittlin ; Susan A. Charman ; Jacques Chollet ; Francis C.K. Chiu ; William N. Charman ; Hugues Matile ; Heinrich Urwyler ; Arnulf Dorn ; et al.
- 关键词：1 ; 2 ; 4-Trioxolanes ; Secondary ozonides ; Antimalarial ; Peroxide ; Artemisinin
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2007
- 出版时间：1 March 2007
- 年：2007
- 卷：17
- 期：5
- 页码：1260-1265
- 全文大小：263 K
文摘
Thirty weak base 1,2,4-dispiro trioxolanes (secondary ozonides) were synthesized. Amino amide trioxolanes had the best combination of antimalarial and biopharmaceutical properties. Guanidine, aminoxy, and amino acid trioxolanes had poor antimalarial activity. Lipophilic trioxolanes were less stable metabolically than their more polar counterparts.