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Trioxanes antiparasitaires : mécanisme d'action et nouvelles molécules biologiquement actives.

Abstract : Discovery of antimalarial and antischistosomiasis properties of artemisinin, extracted from a wormwood, highlights a new family of active compounds: trioxanes. Reduced metallic species mediate oxidative reduction of the peroxide function and transform these trioxanes into heme-alkylating agents. Alkylating properties of artemisin derivatives toward heme, relased from hemoglobine digestion by Plasmodium, were studdied. Schistosomiasis is one of the most prevalent parasitic infections caused by Schistosoma. Praziquantel is actually the only drug active against all schistosome species. Parasites digest host hemoglobin and generate an heme aggregate similar to hemozoin, a pigment formed by Plasmodium. Artemisinin derivatives display a significant activity against Schistosoma. New dual molecules, named trioxaquantels, associating covalently a trioxane to the pirazinoisoquinolin of praziquantel, were synthesized and their biological activities tested on schistosomes.
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https://tel.archives-ouvertes.fr/tel-00567140
Contributor : Sophie Thétiot-Laurent <>
Submitted on : Friday, February 18, 2011 - 1:59:32 PM
Last modification on : Thursday, November 26, 2020 - 11:10:10 AM
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Sophie Thétiot-Laurent. Trioxanes antiparasitaires : mécanisme d'action et nouvelles molécules biologiquement actives.. Autre. Université Paul Sabatier - Toulouse III, 2006. Français. ⟨tel-00567140⟩

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