Weak Base Dispiro-1,2,4-Trioxolanes: Potent Antimalarial Ozonides
- 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.
Publication date
January 2007
DOI Publisher
DigitalCommons@University of Nebraska - Lincoln ISSN
0931-7597 Language
EnglishAbstract
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
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