The comparative antimalarial properties of weak base and neutral synthetic ozonides

Yuanqing Tang, Sergio Wittlin, Susan Ann Charman, Jacques Chollet, Francis Chi Keung Chiu, Julia Morizzi, Lisa Johnson, Josefina Santo Tomas, Christian Scheurer, Christopher Snyder, Lin Zhou, Yuxiang Dong, William Neil Charman, Hugues Matile, Heinrich Urwyler, Arnulf Dorn, Jonathan Vennerstrom

Research output: Contribution to journalArticleResearchpeer-review

11 Citations (Scopus)

Abstract

Thirty-three N-acyl 1,2,4-dispiro tioxolanes (secondary ozonides) were synthesised. For these ozonides, weak base function groups were not required for high antimalarial potency against plasmodium falciparum in vitro, but were necessary for high antimalarial efficacy in plasmodium berghei-infected mice. A wide range of Log p/d ph7.4 values were tolerated, although more liophilic ozonides tended to be less metabolically stable.
Original languageEnglish
Pages (from-to)563 - 566
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume20
Issue number2
DOIs
Publication statusPublished - 2010

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