Literature DB >> 1524966

In vitro activity of the enantiomers of mefloquine, halofantrine and enpiroline against Plasmodium falciparum.

L K Basco1, C Gillotin, F Gimenez, R Farinotti, J Le Bras.   

Abstract

The in vitro activity of the enantiomers of mefloquine, halofantrine and enpiroline was compared against chloroquine-resistant and -susceptible strains of Plasmodium falciparum using a semi-micro drug susceptibility test. For each strain, the corresponding enantiomers exhibited similar activities. The enantiomers of halofantrine were the most active against both susceptible and resistant strains, followed by the enantiomers of mefloquine and enpiroline.

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Year:  1992        PMID: 1524966      PMCID: PMC1381440          DOI: 10.1111/j.1365-2125.1992.tb04081.x

Source DB:  PubMed          Journal:  Br J Clin Pharmacol        ISSN: 0306-5251            Impact factor:   4.335


  11 in total

1.  A comparison of the antimalarial activity of the cinchona alkaloids against Plasmodium falciparum in vitro.

Authors:  D L Wesche; J Black
Journal:  J Trop Med Hyg       Date:  1990-06

2.  Crystal and molecular structure of the antimalarial agent enpiroline.

Authors:  J M Karle; I L Karle
Journal:  Antimicrob Agents Chemother       Date:  1989-07       Impact factor: 5.191

3.  Optical isomers of aryl-2-piperidylmethanol antimalarial agents. Preparation, optical purity, and absolute stereochemistry.

Authors:  F I Carroll; J T Blackwell
Journal:  J Med Chem       Date:  1974-02       Impact factor: 7.446

4.  In vitro activity of chloroquine, the two enantiomers of chloroquine, desethylchloroquine and pyronaridine against Plasmodium falciparum.

Authors:  S Fu; A Björkman; B Wåhlin; D Ofori-Adjei; O Ericsson; F Sjöqvist
Journal:  Br J Clin Pharmacol       Date:  1986-07       Impact factor: 4.335

5.  Determination of the enantiomers of mefloquine in plasma and whole blood using a coupled achiral-chiral high-performance liquid chromatographic system.

Authors:  F Gimenez; R Farinotti; A Thuillier; G Hazebroucq; I W Wainer
Journal:  J Chromatogr       Date:  1990-08-03

6.  Evaluation of the 4-pyridinemethanol WR 180,409 (enpiroline) in the treatment of induced Plasmodium falciparum infections in healthy, non-immune subjects.

Authors:  T M Cosgriff; E F Boudreau; C L Pamplin; J D Berman; M J Shmuklarsky; C J Canfield
Journal:  Am J Trop Med Hyg       Date:  1984-09       Impact factor: 2.345

7.  Antimalarial activities of various 4-quinolonemethanols with special attention to WR-142,490 (mefloquine).

Authors:  L H Schmidt; R Crosby; J Rasco; D Vaughan
Journal:  Antimicrob Agents Chemother       Date:  1978-06       Impact factor: 5.191

8.  Resolution of antimalarial agents via complex formation with alpha-(2,4,5,7-tetranitro-9-fluorenylideneaminooxy) propionic acid.

Authors:  F I Carroll; B Berrang; C P Linn
Journal:  J Med Chem       Date:  1978-04       Impact factor: 7.446

9.  Human malaria parasites in continuous culture.

Authors:  W Trager; J B Jensen
Journal:  Science       Date:  1976-08-20       Impact factor: 47.728

10.  In vitro study of drug sensitivity of Plasmodium falciparum: evaluation of a new semi-micro test.

Authors:  J Le Bras; P Deloron
Journal:  Am J Trop Med Hyg       Date:  1983-05       Impact factor: 2.345

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  21 in total

1.  Antischistosomal activities of mefloquine-related arylmethanols.

Authors:  Katrin Ingram; William Ellis; Jennifer Keiser
Journal:  Antimicrob Agents Chemother       Date:  2012-04-02       Impact factor: 5.191

2.  Case Study of Small Molecules As Antimalarials: 2-Amino-1-phenylethanol (APE) Derivatives.

Authors:  María J Chaparro; Jaume Vidal; Iñigo Angulo-Barturen; José M Bueno; Jeremy Burrows; Nicholas Cammack; Pablo Castañeda; Gonzalo Colmenarejo; José M Coterón; Laura de Las Heras; Esther Fernández; Santiago Ferrer; Raquel Gabarró; Francisco J Gamo; Mercedes García; María B Jiménez-Díaz; María J Lafuente; María L León; María S Martínez; Douglas Minick; Sara Prats; Margarita Puente; Lourdes Rueda; Elena Sandoval; Angel Santos-Villarejo; Michael Witty; Félix Calderón
Journal:  ACS Med Chem Lett       Date:  2014-03-26       Impact factor: 4.345

3.  The stereoselective distribution of halofantrine enantiomers within human, dog, and rat plasma lipoproteins.

Authors:  D R Brocks; M Ramaswamy; A I MacInnes; K M Wasan
Journal:  Pharm Res       Date:  2000-04       Impact factor: 4.200

4.  In vitro efficacy of dicationic compounds and mefloquine enantiomers against Echinococcus multilocularis metacestodes.

Authors:  Britta Stadelmann; Tatiana Küster; Sabrina Scholl; Fabienne Barna; Christian Kropf; Jennifer Keiser; David W Boykin; Chad E Stephens; Andrew Hemphill
Journal:  Antimicrob Agents Chemother       Date:  2011-07-18       Impact factor: 5.191

5.  An investigation of the interaction between halofantrine, CYP2D6 and CYP3A4: studies with human liver microsomes and heterologous enzyme expression systems.

Authors:  R C Halliday; B C Jones; D A Smith; N R Kitteringham; B K Park
Journal:  Br J Clin Pharmacol       Date:  1995-10       Impact factor: 4.335

6.  In vitro and in vivo efficacies of mefloquine-based treatment against alveolar echinococcosis.

Authors:  Tatiana Küster; Britta Stadelmann; Corina Hermann; Sabrina Scholl; Jennifer Keiser; Andrew Hemphill
Journal:  Antimicrob Agents Chemother       Date:  2010-12-06       Impact factor: 5.191

7.  A randomized, double-blind, placebo-controlled study to investigate the safety, tolerability, and pharmacokinetics of single enantiomer (+)-mefloquine compared with racemic mefloquine in healthy persons.

Authors:  Robert Tansley; Julie Lotharius; Anthony Priestley; Fiona Bull; Stephan Duparc; Jörg Möhrle
Journal:  Am J Trop Med Hyg       Date:  2010-12       Impact factor: 2.345

Review 8.  Mefloquine. A review of its antimalarial activity, pharmacokinetic properties and therapeutic efficacy.

Authors:  K J Palmer; S M Holliday; R N Brogden
Journal:  Drugs       Date:  1993-03       Impact factor: 9.546

9.  Plasma concentrations of the enantiomers of halofantrine and its main metabolite in malaria patients.

Authors:  F Gimenez; C Gillotin; L K Basco; O Bouchaud; A F Aubry; I W Wainer; J Le Bras; R Farinotti
Journal:  Eur J Clin Pharmacol       Date:  1994       Impact factor: 2.953

Review 10.  Stereoselectivity in the pharmacodynamics and pharmacokinetics of the chiral antimalarial drugs.

Authors:  Dion R Brocks; Reza Mehvar
Journal:  Clin Pharmacokinet       Date:  2003       Impact factor: 6.447

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