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Novel spiroanellated 1,2,4-trioxanes with high in vitro antimalarial activities
Authors:Griesbeck Axel G  El-Idreesy Tamer T  Höinck Lars-Oliver  Lex Johann  Brun Reto
Affiliation:1. Namık Kemal University, Faculty of Medicine, Department of Pharmacology, 59030 Tekirdag, Turkey;2. Kocaeli University, Faculty of Medicine, Department of Histology and Embryology, Umuttepe 41380, Kocaeli, Turkey;3. Kocaeli University, Faculty of Medicine, Department of Physiology, Umuttepe 41380, Kocaeli, Turkey;4. Kocaeli University, Faculty of Medicine, Department of Pharmacology and Experimental Medical Research and Application Unit, Umuttepe 41380, Kocaeli, Turkey
Abstract:A remarkable increase in antimalarial in vitro activity was achieved by integration of spiroadamantane motifs in 6-alkylidene 1,2,4-trioxanes 3a-h via diastereoselective photooxygenation of allylic alcohols and subsequent BF(3)-catalyzed peroxyacetalization with adamantanone to give the active compounds 3e-h.
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