sample of publications

• articles 

  • Determination of the pharmacokinetics and pharmacodynamics of Isoniazid, Rifampicin, Pyrazinamide and Ethambutol in a cross-over cynomolgus macaque model of Mycobacterium tuberculosis infection.  Pharmaceutics.  14:1-21. 2022
  • Pharmacokinetic / pharmacodynamic relationships of liposomal amphotericin b and miltefosine in experimental visceral leishmaniasis.  PLoS Neglected Tropical Diseases.  15:1-16. 2021
  • A novel class of fast-acting antimalarial agents: Substituted 15-membered azalides.  BRITISH JOURNAL OF PHARMACOLOGY.  178:363-377. 2021
  • Lead optimization of a pyrrole-based dihydroorotate dehydrogenase inhibitor series for the treatment of malaria.  JOURNAL OF MEDICINAL CHEMISTRY.  63. 2020
  • Identification of GSK3186899/DDD853651 as a Preclinical Development Candidate for the Treatment of Visceral Leishmaniasis.  JOURNAL OF MEDICINAL CHEMISTRY.  62. 2019
  • Synthesis and profiling of benzylmorpholine 1,2,4,5-tetraoxane analogue N205: Towards tetraoxane scaffolds with potential for single dose cure of malaria.  BIOORGANIC & MEDICINAL CHEMISTRY.  26:2996-3005. 2018
  • Identification of Fast-Acting 2,6-Disubstituted Imidazopyridines That Are Efficacious in the in Vivo Humanized Plasmodium falciparum NODscidIL2R?null Mouse Model of Malaria.  JOURNAL OF MEDICINAL CHEMISTRY.  61:4213-4227. 2018
  • Synthesis and Structure&-Activity Relationships of the Novel Antimalarials 5-Pyridinyl-4(1H)-Pyridones.  JOURNAL OF MEDICINAL CHEMISTRY.  61:3422-3435. 2018
  • A human microdose study of the antimalarial drug GSK3191607 in healthy volunteers.  BRITISH JOURNAL OF CLINICAL PHARMACOLOGY.  84:482-489. 2018
  • A potent series targeting the malarial cGMP-dependent protein kinase clears infection and blocks transmission.  Nature Communications.  8:1-9. 2017
  • The Discovery of Novel Antimalarial Aminoxadiazoles as a Promising Nonendoperoxide Scaffold.  JOURNAL OF MEDICINAL CHEMISTRY.  60:6880-6896. 2017
  • A tetraoxane-based antimalarial drug candidate that overcomes PfK13-C580Y dependent artemisinin resistance.  Nature Communications.  8:1-10. 2017
  • Antimalarial efficacy of MMV390048, an inhibitor of Plasmodium phosphatidylinositol 4-kinase.  Science Translational Medicine.  9. 2017
  • The multistate tuberculosis pharmacometric model: a semi-mechanistic pharmacokinetic-pharmacodynamic model for studying drug effects in an acute tuberculosis mouse model.  JOURNAL OF PHARMACOKINETICS AND PHARMACODYNAMICS.  44:133-141. 2017
  • A Triazolopyrimidine-Based Dihydroorotate Dehydrogenase Inhibitor with Improved Drug-like Properties for Treatment and Prevention of Malaria.  ACS Infectious Diseases.  2:892-979. 2016
  • Identification of a Potential Antimalarial Drug Candidate from a Series of 2-Aminopyrazines by Optimization of Aqueous Solubility and Potency across the Parasite Life Cycle.  JOURNAL OF MEDICINAL CHEMISTRY.  59:9890-9905. 2016
  • Population pharmacokinetics, optimised design and sample size determination for rifampicin, isoniazid, ethambutol and pyrazinamide in the mouse.  EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES.  93:319-333. 2016
  • Characterization of Novel Antimalarial Compound ACT-451840: Preclinical Assessment of Activity and Dose-Efficacy Modeling.  PLOS MEDICINE.  13. 2016
  • Repurposing clinically approved cephalosporins for tuberculosis therapy.  Scientific Reports.  6. 2016
  • Trisubstituted Pyrimidines as Efficacious and Fast-Acting Antimalarials.  JOURNAL OF MEDICINAL CHEMISTRY.  59:6101-6120. 2016
  • Tetrahydro-2-naphthyl and 2-Indanyl Triazolopyrimidines Targeting Plasmodium falciparum Dihydroorotate Dehydrogenase Display Potent and Selective Antimalarial Activity.  JOURNAL OF MEDICINAL CHEMISTRY.  59. 2016
  • Linking murine and human Plasmodium falciparum challenge models in a translational path for antimalarial drug development.  ANTIMICROBIAL AGENTS AND CHEMOTHERAPY.  60:3669-3675. 2016
  • A novel pyrazolopyridine with in vivo activity in Plasmodium berghei- and Plasmodium falciparum-infected mouse models from structure-activity relationship studies around the core of recently identified antimalarial imidazopyridazines.  JOURNAL OF MEDICINAL CHEMISTRY.  58:8713-8722. 2015
  • Correction for Jiménez-Díaz et al., (+)-SJ733, a clinical candidate for malaria that acts through ATP4 to induce rapid host-mediated clearance of Plasmodium.  PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA.  112:E5764-E5764. 2015
  • A long-duration dihydroorotate dehydrogenase inhibitor (DSM265) for prevention and treatment of malaria.  Science Translational Medicine.  7. 2015
  • A novel multiple-stage antimalarial agent that inhibits protein synthesis.  NATURE.  522. 2015
  • Pharmacokinetic-pharmacodynamic and dose-response relationships of antituberculosis drugs: recommendations and standards for industry and academia.  JOURNAL OF INFECTIOUS DISEASES.  211:S96-S106. 2015
  • Histone methyltransferase inhibitors are orally bioavailable, fast-acting molecules with activity against different species causing malaria in humans.  ANTIMICROBIAL AGENTS AND CHEMOTHERAPY.  59:950-959. 2015
  • (+)-SJ733, a clinical candidate for malaria that acts through ATP4 to induce rapid host-mediated clearance of Plasmodium.  PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA.  111:E5455-E5462. 2014
  • N-aryl-2-aminobenzimidazoles: Novel, efficacious, antimalarial lead compounds.  JOURNAL OF MEDICINAL CHEMISTRY.  57. 2014
  • Aminoazabenzimidazoles, a Novel Class of Orally Active Antimalarial Agents.  JOURNAL OF MEDICINAL CHEMISTRY.  57:5702-5713. 2014
  • Case study of small molecules as antimalarials: 2-amino-1-phenylethanol (APE) derivatives.  ACS Medicinal Chemistry Letters.  5:657-661. 2014
  • Repositioning: the fast track to new anti-malarial medicines?.  MALARIA JOURNAL.  13:1-15. 2014
  • Pyrazoleamide compounds are potent antimalarials that target Na+ homeostasis in intraerythrocytic Plasmodium falciparum.  Nature Communications.  5:1-10. 2014
  • Erratum: Potent antimalarial 4-pyridones with improved physico-chemical properties (Bioorganic and Medicinal Chemistry Letters (2011) 21 (5214-5218)).  Bioorganic and Medicinal Chemistry Letters.  23. 2013
  • Humanised models of infection in the evaluation of anti-malarial drugs.  Drug Discovery Today: Technologies.  10:e351-e357. 2013
  • A new in vivo screening paradigm to accelerate antimalarial drug discovery.  PLoS One.  8:1-12. 2013
  • Quinolone-3-diarylethers: A new class of antimalarial drug.  Science Translational Medicine.  5. 2013
  • Exploration of 4(1H)-pyridones as a novel family of potent antimalarial inhibitors of the plasmodial cytochrome bc1.  Future Medicinal Chemistry.  4:2311-2323. 2012
  • Novel hybrid molecules based on 15-membered azalide as potential antimalarial agents.  EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY.  49:365-378. 2012
  • 4-Substituted Thioquinolines and Thiazoloquinolines: Potent, Selective, and Tween-80 invitro Dependent Families of Antitubercular Agents with Moderate invivo Activity.  ChemMedChem.  6:2252-2263. 2011
  • Potent antimalarial 4-pyridones with improved physico-chemical properties.  Bioorganic and Medicinal Chemistry Letters.  21. 2011
  • Structure-guided lead optimization of triazolopyrimidine-ring substituents identifies potent plasmodium falciparum dihydroorotate dehydrogenase inhibitors with clinical candidate potential.  JOURNAL OF MEDICINAL CHEMISTRY.  54:5540-5561. 2011
  • Aminoindoles, a Novel Scaffold with Potent Activity against Plasmodium falciparum.  ANTIMICROBIAL AGENTS AND CHEMOTHERAPY.  55:2612-2622. 2011
  • Chemical genetics of Plasmodium falciparum.  NATURE.  465. 2010