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Preparation and antimalarial activities of "trioxaquines", new modular molecules with a trioxane skeleton linked to a 4-aminoquinoline.
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TLDR
This strategy, which can be characterized as a “covalent bitherapy”, allowed us to obtain modular molecules with high antimalarial activity in vitro either on chloroquine sensitive or onchloroquine resistant Plasmodium falciparum strains.Abstract:
Trioxaquines are new antimalarial drugs which combine two active fragments (an aminoquinoline and a trioxane) with independant modes of action covalently linked within a single molecule. This strategy, which can be characterized as a “covalent bitherapy”, allowed us to obtain modular molecules with high antimalarial activity in vitro either on chloroquine sensitive or on chloroquine resistant Plasmodium falciparum strains.read more
Citations
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Photochemical Reactions as Key Steps in Organic Synthesis
TL;DR: Photochemical Electron-Transfer Reactions with a Catalytic Sensitizer 1068 6.1.1 Photochemical Extrusion of Small Molecules 1067 6.2.2 Photochemical Rearrangings 1061 4.4.3.
Journal ArticleDOI
Hybrid molecules with a dual mode of action: dream or reality?
TL;DR: In order to obtain new antimalarial drugs that are affordable and able to avoid the emergence of resistant strains, the authors developed hybrid molecules with a dual mode of action able to kill multiresistant strains by oral administration.
Journal ArticleDOI
A medicinal chemistry perspective on artemisinin and related endoperoxides.
Paul M. O'Neill,Gary H. Posner +1 more
TL;DR: The explicit mechanism depicted in Scheme 1 is supported by the work of Berman and Adams and others, and it was proposed that the damage caused to the parasite’s FV membrane leads to vacuolar rupture and parasite autodigestion.
Journal ArticleDOI
Drug discovery and development for neglected parasitic diseases
Adam R. Renslo,James H. McKerrow +1 more
TL;DR: This review will summarize efforts to reinvigorate the drug development pipeline for tropical parasites, which is driven in large part by support from major philanthropies.
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From mechanistic studies on artemisinin derivatives to new modular antimalarial drugs.
TL;DR: Some possible ways for discovery of new drugs, especially the design of trioxaquines, new active molecules recently patented that have been prepared by covalent attachment of a trioxane residue having alkylating ability to a quinoline moiety known to easily penetrate within infected erythrocytes, are presented.
References
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Journal ArticleDOI
Human malaria parasites in continuous culture
William Trager,James B. Jensen +1 more
TL;DR: Plasmodium falciparum can now be maintained in continuous culture in human erythrocytes incubated at 38 degrees C in RPMI 1640 medium with human serum under an atmosphere with 7 percent carbon dioxide and low oxygen.
Journal ArticleDOI
Synchronization of Plasmodium falciparum erythrocytic stages in culture.
TL;DR: Synchronous development of the erythrocytic stages of a human malaria parasite, Plasmodium falciparum, in culture was accomplished by suspending cultured parasites in 5% D-sorbitol and subsequent reintroduction into culture.
Journal ArticleDOI
Quantitative assessment of antimalarial activity in vitro by a semiautomated microdilution technique.
TL;DR: A rapid, semiautomated microdilution method was developed for measuring the activity of potential antimalarial drugs against cultured intraerythrocytic asexual forms of the human malaria parasite Plasmodium falciparum, and results demonstrated that the method is sensitive and precise.
Journal ArticleDOI
Averting a malaria disaster.
Nicholas J. White,François Nosten,Sornchai Looareesuwan,William M. Watkins,Kevin Marsh,Robert W. Snow,Gilbert Kokwaro,John H. Ouma,Tran Tinh Hien,Malcolm E. Molyneux,Malcolm E. Molyneux,Terrie E. Taylor,Terrie E. Taylor,Chris I. Newbold,TK Ruebush,M Danis,Brian Greenwood,Roy M. Anderson,Piero Olliaro +18 more
TL;DR: Pyrimethamine-sulphadoxine (PSD) is usually deployed as a successor to chloroquine, but resistance to PSD is increasing and a health calamity looms within the next few years.
Journal ArticleDOI
Cytotoxic and antimalarial bisbenzylisoquinoline alkaloids from Stephania erecta.
Kittisak Likhitwitayawuid,Cindy K. Angerhofer,Geoffrey A. Cordell,John M. Pezzuto,Nijsiri Ruangrungsi +4 more
TL;DR: (+)-2-N-Methyltelobine, a new alkaloid, together with twelve known bisbenzylisoquinolines, was isolated from the tubers of Stephania erecta and did not appear to be promising clinical candidates at the present time.
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