期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 17, 期 5, 页码 1260-1265出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.12.007
关键词
1,2,4-trioxolanes; secondary ozonides; antimalarial; peroxide; artemisinin
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.
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