Lluis Ballell

Summary

Affiliation: GlaxoSmithKline Research and Development
Country: USA

Publications

  1. pmc Fueling open-source drug discovery: 177 small-molecule leads against tuberculosis
    Lluis Ballell
    Tres Cantos Medicines Development Campus TCMDC, GlaxoSmithKline GSK, Severo Ochoa 2, Tres Cantos, Madrid, Spain
    ChemMedChem 8:313-21. 2013
  2. ncbi request reprint New thiopyrazolo[3,4-d]pyrimidine derivatives as anti-mycobacterial agents
    Lluis Ballell
    Centre for Carbohydrate Chemistry, School of Chemical Sciences and Pharmacy, University of East Anglia, Norwich, NR4 7TJ, UK
    Bioorg Med Chem Lett 17:1736-40. 2007
  3. pmc Antitubercular drugs for an old target: GSK693 as a promising InhA direct inhibitor
    María Martínez-Hoyos
    Diseases of the Developing World, GlaxoSmithKline, Severo Ochoa 2, 28760 Tres Cantos, Madrid, Spain
    EBioMedicine 8:291-301. 2016
  4. pmc Tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide and N-benzyl-6',7'-dihydrospiro[piperidine-4,4'-thieno[3,2-c]pyran] analogues with bactericidal efficacy against Mycobacterium tuberculosis targeting MmpL3
    Modesto J Remuiñán
    Diseases of the Developing World, GlaxoSmithKline, Tres Cantos, Madrid, Spain
    PLoS ONE 8:e60933. 2013
  5. pmc Mycobacterium tuberculosis gyrase inhibitors as a new class of antitubercular drugs
    Delia Blanco
    Diseases of the Developing World, GSK, Severo Ochoa 2, Tres Cantos, Madrid, Spain
    Antimicrob Agents Chemother 59:1868-75. 2015
  6. doi request reprint 4-Substituted thioquinolines and thiazoloquinolines: potent, selective, and Tween-80 in vitro dependent families of antitubercular agents with moderate in vivo activity
    Jaime Escribano
    Diseases of the Developing World DDW, Tres Cantos Medicines Development Campus TCMDC, GlaxoSmithKline, Severo Ochoa 2, 28760 Tres Cantos Madrid, Spain
    ChemMedChem 6:2252-63. 2011
  7. pmc Release of 50 new, drug-like compounds and their computational target predictions for open source anti-tubercular drug discovery
    María José Rebollo-Lopez
    Diseases of the Developing World, GlaxoSmithKline, Tres Cantos, Madrid, Spain
    PLoS ONE 10:e0142293. 2015
  8. pmc Combinations of β-Lactam Antibiotics Currently in Clinical Trials Are Efficacious in a DHP-I-Deficient Mouse Model of Tuberculosis Infection
    Joaquín Rullas
    Diseases of the Developing World, GlaxoSmithKline, Tres Cantos, Madrid, Spain Open Collaborative Model for Tuberculosis Lead Optimisation ORCHID Consortium
    Antimicrob Agents Chemother 59:4997-9. 2015
  9. ncbi request reprint Synthesis and evaluation of mimetics of UDP and UDP-alpha-D-galactose, dTDP and dTDP-alpha-D-glucose with monosaccharides replacing the key pyrophosphate unit
    Lluis Ballell
    Centre for Carbohydrate Chemistry, School of Chemical Sciences and Pharmacy, University of East Anglia, Norwich, UK NR4 7TJ
    Org Biomol Chem 3:1109-15. 2005
  10. pmc New small-molecule synthetic antimycobacterials
    Lluis Ballell
    Pharmaceutical Sciences Faculty, Medicinal Chemistry Group, Sorbonnelaan 16, Utrecht University, Utrecht 3584 CA, The Netherlands
    Antimicrob Agents Chemother 49:2153-63. 2005

Collaborators

  • Neeraj Dhar
  • Robert A Field
  • Robert J Young
  • M Soledad Jimenez
  • Vinod Kumar
  • James R Brown
  • Gurdyal S Besra
  • Douglas J Minick
  • David J Dow
  • Marc A Marti-Renom
  • Ken Duncan
  • Inigo Angulo-Barturen
  • María Martínez-Hoyos
  • Joaquín Rullas
  • Esther Pérez-Herrán
  • David Barros
  • Alfonso Mendoza-Losana
  • María José Rebollo-Lopez
  • Julia Castro-Pichel
  • Modesto J Remuiñán
  • John D McKinney
  • Daniel Alvarez-Gomez
  • Jose Luis Lavandera
  • Adolfo García-Pérez
  • Delia Blanco
  • Joel Lelièvre
  • Rubén González Del Río
  • Nicholas Cammack
  • Monica Cacho
  • Santiago Ferrer-Bazaga
  • Jaime Escribano
  • Silvia González Del Valle
  • Gulcin Gulten
  • Sophie Huss
  • Emilio Alvarez
  • Pedro Torres
  • José Francisco García-Bustos
  • Lourdes Encinas
  • Fátima Ortega
  • James C Sacchettini
  • Pablo Castañeda
  • Delia Blanco Ruano
  • Nuria Martin-Casabona
  • Sundip Modha
  • François Signorino-Gelo
  • Joaquin Rullas-Trincado
  • Raquel Fernández Menéndez
  • Ermias Woldu
  • Michel Arthur
  • Emilio Alvarez-Ruiz
  • Julia Castro
  • Mark Hurle
  • Jean Emmanuel Hugonnet
  • Alfonso Mendoza
  • John P Overington
  • Gonzalo Colmenarejo
  • Eva Maria Lopez-Roman
  • Grace Mugumbate
  • María Cleofé Zapatero-González
  • Andreas H Diacon
  • María Jesús Vázquez-Muñiz
  • Cindy Richards
  • George Papadatos
  • Francisco Martínez-Jiménez
  • Robert H Bates
  • Vanessa Barroso
  • David Barros-Aguirre
  • David Barros-Aguire
  • Jorge Esquivias
  • Carlos Alemparte
  • Nalini Mehta
  • Elena Jimenez
  • Verónica Sousa
  • Nicholas J Loman
  • Mark J Pallen
  • Vickey L Spivey
  • María Teresa Fraile-Gabaldón
  • Johnson Afari
  • Chrystala Constantinidou
  • Carolina Gonzalez
  • Fátima Ortega-Muro
  • Hilda Rivera
  • Cristina Rivero-Hernández
  • Elena Jiménez-Navarro

Detail Information

Publications11

  1. pmc Fueling open-source drug discovery: 177 small-molecule leads against tuberculosis
    Lluis Ballell
    Tres Cantos Medicines Development Campus TCMDC, GlaxoSmithKline GSK, Severo Ochoa 2, Tres Cantos, Madrid, Spain
    ChemMedChem 8:313-21. 2013
    ..Two additional drug-discovery-relevant datasets are included: a) a drug-like property analysis reflecting the latest lead-like guidelines and b) an early lead-generation package of the most promising hits within the clusters identified...
  2. ncbi request reprint New thiopyrazolo[3,4-d]pyrimidine derivatives as anti-mycobacterial agents
    Lluis Ballell
    Centre for Carbohydrate Chemistry, School of Chemical Sciences and Pharmacy, University of East Anglia, Norwich, NR4 7TJ, UK
    Bioorg Med Chem Lett 17:1736-40. 2007
    ..These compounds showed significant anti-mycobacterial activity (MICs down to 2mug/ml) and their potential as significant drug-like leads is substantiated through cytotoxicity evaluation and in silico profiling...
  3. pmc Antitubercular drugs for an old target: GSK693 as a promising InhA direct inhibitor
    María Martínez-Hoyos
    Diseases of the Developing World, GlaxoSmithKline, Severo Ochoa 2, 28760 Tres Cantos, Madrid, Spain
    EBioMedicine 8:291-301. 2016
    ..Here, we present a series of InhA DI active against multidrug (MDR) and extensively (XDR) drug-resistant clinical isolates as well as in TB murine models when orally dosed that can be a promising foundation for a future treatment. ..
  4. pmc Tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide and N-benzyl-6',7'-dihydrospiro[piperidine-4,4'-thieno[3,2-c]pyran] analogues with bactericidal efficacy against Mycobacterium tuberculosis targeting MmpL3
    Modesto J Remuiñán
    Diseases of the Developing World, GlaxoSmithKline, Tres Cantos, Madrid, Spain
    PLoS ONE 8:e60933. 2013
    ..In vivo efficacy evaluation of two optimized THPP and Spiro leads showed how the compounds were able to reduce >2 logs bacterial cfu counts in the lungs of infected mice...
  5. pmc Mycobacterium tuberculosis gyrase inhibitors as a new class of antitubercular drugs
    Delia Blanco
    Diseases of the Developing World, GSK, Severo Ochoa 2, Tres Cantos, Madrid, Spain
    Antimicrob Agents Chemother 59:1868-75. 2015
    ..The remarkable in vitro and in vivo antitubercular profiles showed by the hits has prompted us to further advance the MGI project to full lead optimization. ..
  6. doi request reprint 4-Substituted thioquinolines and thiazoloquinolines: potent, selective, and Tween-80 in vitro dependent families of antitubercular agents with moderate in vivo activity
    Jaime Escribano
    Diseases of the Developing World DDW, Tres Cantos Medicines Development Campus TCMDC, GlaxoSmithKline, Severo Ochoa 2, 28760 Tres Cantos Madrid, Spain
    ChemMedChem 6:2252-63. 2011
    ..Although the final compounds showed only limited levels of systemic exposure in mice, modest levels of efficacy in vivo at nontoxic doses were observed...
  7. pmc Release of 50 new, drug-like compounds and their computational target predictions for open source anti-tubercular drug discovery
    María José Rebollo-Lopez
    Diseases of the Developing World, GlaxoSmithKline, Tres Cantos, Madrid, Spain
    PLoS ONE 10:e0142293. 2015
    ..This effort has resulted in the identification of novel compounds and their hypothesized targets that will hopefully fuel future TB drug discovery and target validation programs alike. ..
  8. pmc Combinations of β-Lactam Antibiotics Currently in Clinical Trials Are Efficacious in a DHP-I-Deficient Mouse Model of Tuberculosis Infection
    Joaquín Rullas
    Diseases of the Developing World, GlaxoSmithKline, Tres Cantos, Madrid, Spain Open Collaborative Model for Tuberculosis Lead Optimisation ORCHID Consortium
    Antimicrob Agents Chemother 59:4997-9. 2015
    ..These findings provide evidence supporting the potential of β-lactams as safe and mycobactericidal components of new combination regimens against TB with or without resistance to currently used drugs. ..
  9. ncbi request reprint Synthesis and evaluation of mimetics of UDP and UDP-alpha-D-galactose, dTDP and dTDP-alpha-D-glucose with monosaccharides replacing the key pyrophosphate unit
    Lluis Ballell
    Centre for Carbohydrate Chemistry, School of Chemical Sciences and Pharmacy, University of East Anglia, Norwich, UK NR4 7TJ
    Org Biomol Chem 3:1109-15. 2005
    ..These compounds proved not to be inhibitors of bovine beta-1,4-galactosyltransferase although some showed moderate inhibition of Salmonella dTDP-alpha-D-glucose 4,6-dehydratase (RmlB)...
  10. pmc New small-molecule synthetic antimycobacterials
    Lluis Ballell
    Pharmaceutical Sciences Faculty, Medicinal Chemistry Group, Sorbonnelaan 16, Utrecht University, Utrecht 3584 CA, The Netherlands
    Antimicrob Agents Chemother 49:2153-63. 2005
  11. ncbi request reprint A new chemical probe for the detection of the cancer-linked galectin-3
    Lluis Ballell
    Department of Medicinal Chemistry and Chemical Biology, Utrecht Institute for Pharmaceutical Sciences, Utrecht University, PO Box 80082, 3508 TB, Utrecht, The Netherlands
    Org Biomol Chem 4:4387-94. 2006
    ..Introduction of a fluorescent label via'click' chemistry allows the labelled proteins to be visualized in a gel. With the probe, selective visualization of galectin-3 in protein mixtures was shown and remarkably even in cell lysates...