Literature DB >> 24944739

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

María J Chaparro1, Jaume Vidal1, Iñigo Angulo-Barturen1, José M Bueno1, Jeremy Burrows2, Nicholas Cammack1, Pablo Castañeda1, Gonzalo Colmenarejo3, José M Coterón1, Laura de Las Heras1, Esther Fernández1, Santiago Ferrer1, Raquel Gabarró1, Francisco J Gamo1, Mercedes García1, María B Jiménez-Díaz1, María J Lafuente1, María L León1, María S Martínez1, Douglas Minick4, Sara Prats1, Margarita Puente1, Lourdes Rueda1, Elena Sandoval1, Angel Santos-Villarejo1, Michael Witty2, Félix Calderón1.   

Abstract

Antiparasitic oral drugs have been associated to lipophilic molecules due to their intrinsic permeability. However, these kind of molecules are associated to numerous adverse effects, which have been extensively studied. Within the Tres Cantos Antimalarial Set (TCAMS) we have identified two small, soluble and simple hits that even presenting antiplasmodial activities in the range of 0.4-0.5 μM are able to show in vivo activity.

Entities:  

Keywords:  Aminoalcoholes; TCAMS; malaria; mefloquine; tres cantos antimalarial set

Year:  2014        PMID： 24944739      PMCID： PMC4060931          DOI： 10.1021/ml500015r

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  14 in total

1.  Absolute configuration determination of chiral molecules in the solution state using vibrational circular dichroism.

Authors:  Teresa B Freedman; Xiaolin Cao; Rina K Dukor; Laurence A Nafie
Journal:  Chirality       Date:  2003-11       Impact factor: 2.437

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

Authors:  L K Basco; C Gillotin; F Gimenez; R Farinotti; J Le Bras
Journal:  Br J Clin Pharmacol       Date:  1992-05       Impact factor: 4.335

Review 3.  A lesson learnt: the rise and fall of Lariam and Halfan.

Authors:  Ashley M Croft
Journal:  J R Soc Med       Date:  2007-04       Impact factor: 5.344

4.  Thousands of chemical starting points for antimalarial lead identification.

Authors:  Francisco-Javier Gamo; Laura M Sanz; Jaume Vidal; Cristina de Cozar; Emilio Alvarez; Jose-Luis Lavandera; Dana E Vanderwall; Darren V S Green; Vinod Kumar; Samiul Hasan; James R Brown; Catherine E Peishoff; Lon R Cardon; Jose F Garcia-Bustos
Journal:  Nature       Date:  2010-05-20       Impact factor: 49.962

5.  A Divergent SAR Study Allows Optimization of a Potent 5-HT2c Inhibitor to a Promising Antimalarial Scaffold.

Authors:  Félix Calderón; Jaume Vidal-Mas; Jeremy Burrows; Juan Carlos de la Rosa; María Belén Jiménez-Díaz; Teresa Mulet; Sara Prats; Jorge Solana; Michael Witty; Francisco Javier Gamo; Esther Fernández
Journal:  ACS Med Chem Lett       Date:  2012-02-09       Impact factor: 4.345

Review 6.  Challenges in antimalarial drug discovery.

Authors:  Jeremy N Burrows; Didier Leroy; Julie Lotharius; David Waterson
Journal:  Future Med Chem       Date:  2011-09       Impact factor: 3.808

7.  1H-NMR studies of drugs with chiral solvating agent: the direct enantiomeric purity determination of the chiral anesthetic, prilocaine.

Authors:  G M Hanna
Journal:  Enantiomer       Date:  2000

8.  Artemisinin resistance in Plasmodium falciparum malaria.

Authors:  Arjen M Dondorp; François Nosten; Poravuth Yi; Debashish Das; Aung Phae Phyo; Joel Tarning; Khin Maung Lwin; Frederic Ariey; Warunee Hanpithakpong; Sue J Lee; Pascal Ringwald; Kamolrat Silamut; Mallika Imwong; Kesinee Chotivanich; Pharath Lim; Trent Herdman; Sen Sam An; Shunmay Yeung; Pratap Singhasivanon; Nicholas P J Day; Niklas Lindegardh; Duong Socheat; Nicholas J White
Journal:  N Engl J Med       Date:  2009-07-30       Impact factor: 91.245

9.  A new in vivo screening paradigm to accelerate antimalarial drug discovery.

Authors:  María Belén Jiménez-Díaz; Sara Viera; Javier Ibáñez; Teresa Mulet; Noemí Magán-Marchal; Helen Garuti; Vanessa Gómez; Lorena Cortés-Gil; Antonio Martínez; Santiago Ferrer; María Teresa Fraile; Félix Calderón; Esther Fernández; Leonard D Shultz; Didier Leroy; David M Wilson; José Francisco García-Bustos; Francisco Javier Gamo; Iñigo Angulo-Barturen
Journal:  PLoS One       Date:  2013-06-25       Impact factor: 3.240

10.  P. falciparum in vitro killing rates allow to discriminate between different antimalarial mode-of-action.

Authors:  Laura M Sanz; Benigno Crespo; Cristina De-Cózar; Xavier C Ding; Jose L Llergo; Jeremy N Burrows; Jose F García-Bustos; Francisco-Javier Gamo
Journal:  PLoS One       Date:  2012-02-23       Impact factor: 3.240
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  4 in total

1.  Structure-activity and structure-property relationship studies of spirocyclic chromanes with antimalarial activity.

Authors:  Iredia D Iyamu; Yingzhao Zhao; Prakash T Parvatkar; Bracken F Roberts; Debora R Casandra; Lukasz Wojtas; Dennis E Kyle; Debopam Chakrabarti; Roman Manetsch
Journal:  Bioorg Med Chem       Date:  2022-01-14       Impact factor: 3.461

2.  A small-fish model for behavioral-toxicological screening of new antimalarial drugs: a comparison between erythro- and threo-mefloquine.

Authors:  Hans Maaswinkel; Liqun Zhu; Wei Weng
Journal:  BMC Res Notes       Date:  2015-04-02

3.  Identification and characterization of hundreds of potent and selective inhibitors of Trypanosoma brucei growth from a kinase-targeted library screening campaign.

Authors:  Rosario Diaz; Sandra A Luengo-Arratta; João D Seixas; Emanuele Amata; William Devine; Carlos Cordon-Obras; Domingo I Rojas-Barros; Elena Jimenez; Fatima Ortega; Sabrinia Crouch; Gonzalo Colmenarejo; Jose Maria Fiandor; Jose Julio Martin; Manuela Berlanga; Silvia Gonzalez; Pilar Manzano; Miguel Navarro; Michael P Pollastri
Journal:  PLoS Negl Trop Dis       Date:  2014-10-23

4.  Novel 2-Phenoxyanilide Congeners Derived from a Hit Structure of the TCAMS: Synthesis and Evaluation of Their in Vitro Activity against Plasmodium falciparum.

Authors:  Thomas Weidner; Abed Nasereddin; Lutz Preu; Johann Grünefeld; Ron Dzikowski; Conrad Kunick
Journal:  Molecules       Date:  2016-02-17       Impact factor: 4.411
  4 in total

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