Le Manach C Nchinda AT Paquet T Gonzàlez Cabrera D Younis Y Han Z Bashyam S Zabiulla M Taylor D Lawrence N White KL Charman SA Waterson D Witty MJ Wittlin S Botha ME Nondaba SH Reader J Birkholtz LM Jiménez-Díaz MB Martínez MS Ferrer S Angulo-Barturen I Meister S Antonova-Koch Y Winzeler EA Street LJ Chibale K 2016 Introduction of water-solubilizing groups on the 5-phenyl ring of a 2-aminopyrazine series led to the identification of highly potent compounds against the blood life-cycle stage of the human malaria parasite Plasmodium falciparum. Several compounds displayed high in vivo efficacy in two different mouse models for malaria, P. berghei-infected mice and P. falciparum-infected NOD-scid IL-2Rγnull mice. One of the frontrunners, compound 3, was identified to also have good pharmacokinetics and additionally very potent activity against the liver and gametocyte parasite life-cycle stages. https://sonar.ch/global/documents/231930 eng info:eu-repo/semantics/altIdentifier/doi/10.1021/acs.jmedchem.6b01265 info:eu-repo/semantics/altIdentifier/pmid/27748596 Journal of medicinal chemistry. - 2016 Animals Antimalarials Disease Models, Animal Dose-Response Relationship, Drug Ether-A-Go-Go Potassium Channels Hep G2 Cells Humans Life Cycle Stages Malaria Mice Mice, SCID Microsomes, Liver Molecular Structure Parasitic Diseases, Animal Parasitic Sensitivity Tests Plasmodium berghei Plasmodium falciparum Pyrazines Solubility Structure-Activity Relationship Water 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. http://purl.org/coar/resource_type/c_6501