Journal ArticleDOI
Synthesis and reactions of antimalarial bicyclic peroxides
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This article is published in Journal of Heterocyclic Chemistry.The article was published on 2000-05-01. It has received 24 citations till now. The article focuses on the topics: Bicyclic molecule.read more
Citations
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Journal ArticleDOI
Thiyl Radicals in Organic Synthesis
TL;DR: The thiol−olefin cooxidation process was applied to the total synthesis of antimalarial agent yingzhaosu A and was extended to include the more challenging 1,5-dienes, from which six-membered ring endoperoxides can be obtained.
Journal ArticleDOI
Artemisinin: mechanisms of action, resistance and toxicity.
TL;DR: At high doses, artemisinin can be neurotoxic but toxicity has not been found in clinical studies, and the mechanism of neurotoxicity may be similar to the mechanisms of action.
Journal ArticleDOI
Antimalarial chemotherapeutic peroxides: artemisinin, yingzhaosu A and related compounds.
TL;DR: This review summarises recent achievements in this area of peroxide drug development for malaria chemotherapy in Mechanism-based rational design and gram-scale chemical synthesis.
Journal ArticleDOI
Synthesis of heterocycles by radical cyclisation
TL;DR: In this article, the authors present a review of the work of Perkin Trans. Soc., J. Chem. Trans. 1, 2000, 1, 1], 1.
Journal ArticleDOI
A short synthesis and biological evaluation of potent and nontoxic antimalarial bridged bicyclic beta-sulfonyl-endoperoxides.
Mario D. Bachi,Edward E. Korshin,Roland Hoos,Alex M. Szpilman,Poonsakdi Ploypradith,Suji Xie,Theresa A. Shapiro,Gary H. Posner +7 more
TL;DR: In vivo testing of a few selected peroxides against Plasmodium berghei N indicates that the antimalarial efficacies of beta-sulfonyl peroxide 39a, 46a,46b, and 50a are comparable to those of some of the best antimalaria drugs and are higher than artemisinin against chloroquine-resistant Plas modium yoelii ssp.
References
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Journal ArticleDOI
The base catalyzed decomposition of a dialkyl peroxide
Book ChapterDOI
Antimalarial Activity of Artemisinin (Qinghaosu) and Related Trioxanes: Mechanism (s) of Action
TL;DR: The developing understanding is the mechanism of action in which the endoperoxide linkage is a trigger, activated by iron-induced reduction inside the malaria parasite that releases a cascade of reactive intermediates that ultimately cause fatal damage to the parasites.
Journal ArticleDOI
Mechanism-based design, synthesis, and in vitro antimalarial testing of new 4-methylated trioxanes structurally related to artemisinin: the importance of a carbon-centered radical for antimalarial activity.
Gary H. Posner,Chang Ho Oh,Chang Ho Oh,Chang Ho Oh,Dasong Wang,Dasong Wang,Dasong Wang,Lucia Gerena,Lucia Gerena,Lucia Gerena,Wilbur K. Milhous,Wilbur K. Milhous,Wilbur K. Milhous,Steven R. Meshnick,Wanida Asawamahasadka +14 more
Journal ArticleDOI
Evidence for Fe(IV):O in the Molecular Mechanism of Action of the Trioxane Antimalarial Artemisinin
Journal ArticleDOI
Is alkylation the main mechanism of action of the antimalarial drug artemisinin
Anne Robert,Bernard Meunier +1 more
TL;DR: The characterization of a covalent artemisinin-heme model adduct supports the role of C-centered radicals generated by the reductive activation of the peroxidic bond of this class of drugs.
Related Papers (5)
Thiol-Oxygen Cooxidation of Monoterpenes. Synthesis of Endoperoxides Structurally Related to Antimalarial Yingzhaosu A
Mario D. Bachi,Edward E. Korshin +1 more