Weak base dispiro-1,2,4-trioxolanes: Potent antimalarial ozonides

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:17

Article

Tang, Yuanqing ; Dong, Yuxiang ; Wittlin, Sergio ; Charman, Susan A. ; Chollet, Jacques ; Chiu, Francis C. K. ; Charman, William N. ; Matile, Hugues ; Urwyler, Heinrich ; Dorn, Arnulf ; Bajpai, Saroj ; Wang, Xiaofang ; Padmanilayam, Maniyan ; Karle, Jean M. ; Brun, Reto ; Vennerstrom, Jonathan L.

关键词: 1,2,4-trioxolanes;    secondary ozonides;    antimalarial;    peroxide;    artemisinin;   

DOI  :  10.1016/j.bmcl.2006.12.007

来源: Elsevier

【 摘 要 】

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. (c) 2006 Elsevier Ltd. All rights reserved.

【 授权许可】

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