Literature DB >> 20686674

Antimalarial Preclinical Drug Development: A Single Oral Dose of A 5-Carbon-linked Trioxane Dimer Plus Mefloquine Cures Malaria-Infected Mice.

Deuk Kyu Moon1, Vandana Singhal, Nirbhay Kumar, Theresa A Shapiro, Gary H Posner.   

Abstract

Three new 5-carbon-linked trioxane dimer carboxylate esters have been prepared from the natural trioxane, artemisinin in only 3-steps and 40-50% overall yields. Each one of these new chemical entities is at least as efficacious as the clinically used trioxane antimalarial drug artemether when combined with mefloquine hydrochloride in a low single oral dose cure.

Entities:  

Year:  2009        PMID： 20686674      PMCID： PMC2913489          DOI： 10.1002/ddr.20350

Source DB:  PubMed          Journal:  Drug Dev Res        ISSN： 0272-4391            Impact factor:   4.360


  25 in total

1.  Antitumor activity of novel deoxoartemisinin monomers, dimers, and trimer.

Authors:  Mankil Jung; Sangmin Lee; Jungyeob Ham; Kyunghoon Lee; Hanjo Kim; Soo Kie Kim
Journal:  J Med Chem       Date:  2003-03-13       Impact factor: 7.446

Review 2.  A medicinal chemistry perspective on artemisinin and related endoperoxides.

Authors:  Paul M O'Neill; Gary H Posner
Journal:  J Med Chem       Date:  2004-06-03       Impact factor: 7.446

Review 3.  Artemisinin-based combinations.

Authors:  Elizabeth A Ashley; Nicholas J White
Journal:  Curr Opin Infect Dis       Date:  2005-12       Impact factor: 4.915

Review 4.  Fluoroartemisinins: metabolically more stable antimalarial artemisinin derivatives.

Authors:  Jean-Pierre Bégué; Danièle Bonnet-Delpon
Journal:  ChemMedChem       Date:  2007-05       Impact factor: 3.466

5.  Malaria-infected mice are cured by oral administration of new artemisinin derivatives.

Authors:  Gary H Posner; Wonsuk Chang; Lindsey Hess; Lauren Woodard; Sandra Sinishtaj; Aimee R Usera; William Maio; Andrew S Rosenthal; Alvin S Kalinda; John G D'Angelo; Kimberly S Petersen; Remo Stohler; Jacques Chollet; Josefina Santo-Tomas; Christopher Snyder; Matthias Rottmann; Sergio Wittlin; Reto Brun; Theresa A Shapiro
Journal:  J Med Chem       Date:  2008-01-31       Impact factor: 7.446

Review 6.  Efficacy and safety of dihydroartemisinin-piperaquine.

Authors:  H Y Myint; E A Ashley; N P J Day; F Nosten; N J White
Journal:  Trans R Soc Trop Med Hyg       Date:  2007-07-19       Impact factor: 2.184

7.  Synthesis, antimalarial activity, and intracellular targets of MEFAS, a new hybrid compound derived from mefloquine and artesunate.

Authors:  Fernando de Pilla Varotti; Ana Cristina C Botelho; Anderson Assunção Andrade; Renata C de Paula; Elaine M S Fagundes; Alessandra Valverde; Lúcia M U Mayer; Jorge Souza Mendonça; Marcus V N de Souza; Núbia Boechat; Antoniana Ursine Krettli
Journal:  Antimicrob Agents Chemother       Date:  2008-08-18       Impact factor: 5.191

Review 8.  Qinghaosu (artemisinin): an antimalarial drug from China.

Authors:  D L Klayman
Journal:  Science       Date:  1985-05-31       Impact factor: 47.728

9.  Efficacy and safety of a fixed dose artesunate-sulphamethoxypyrazine-pyrimethamine compared to artemether-lumefantrine for the treatment of uncomplicated falciparum malaria across Africa: a randomized multi-centre trial.

Authors:  Issaka Sagara; Stephen Rulisa; Wilfred Mbacham; Ishag Adam; Kourane Sissoko; Hamma Maiga; Oumar B Traore; Niawanlou Dara; Yahia T Dicko; Alassane Dicko; Abdoulaye Djimdé; F Herwig Jansen; Ogobara K Doumbo
Journal:  Malar J       Date:  2009-04-14       Impact factor: 2.979

10.  Factors related to compliance to anti-malarial drug combination: example of amodiaquine/sulphadoxine-pyrimethamine among children in rural Senegal.

Authors:  Aurélia Souares; Richard Lalou; Ibra Sene; Diarietou Sow; Jean-Yves Le Hesran
Journal:  Malar J       Date:  2009-06-04       Impact factor: 2.979
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  4 in total

1.  3-Alkoxy-1,2-Dioxolanes: Synthesis and Evaluation as Potential Antimalarial Agents.

Authors:  Charles E Schiaffo; Matthias Rottman; Sergio Wittlin; Patrick H Dussault
Journal:  ACS Med Chem Lett       Date:  2011-04-14       Impact factor: 4.345

2.  A single, low, oral dose of a 5-carbon-linked trioxane dimer orthoester plus mefloquine cures malaria-infected mice.

Authors:  Deuk Kyu Moon; Abhai Tripathi; David Sullivan; Maxime A Siegler; Sean Parkin; Gary H Posner
Journal:  Bioorg Med Chem Lett       Date:  2010-09-29       Impact factor: 2.823

3.  Antimalarial chemotherapy: artemisinin-derived dimer carbonates and thiocarbonates.

Authors:  Jennifer R Mazzone; Ryan C Conyers; Abhai K Tripathi; David J Sullivan; Gary H Posner
Journal:  Bioorg Med Chem Lett       Date:  2014-04-16       Impact factor: 2.823

4.  Malaria-Infected Mice Are Cured by a Single Low Dose of a New Silylamide Trioxane Plus Mefloquine.

Authors:  Lauren E Woodard; Bryan T Mott; Vandana Singhal; Nirbhay Kumar; Theresa A Shapiro; Gary H Posner
Journal:  Pharmaceuticals (Basel)       Date:  2009-12-21
  4 in total

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