1450666-66-6Relevant articles and documents
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
Le Manach, Claire,Nchinda, Aloysius T.,Paquet, Tanya,Gonzàlez Cabrera, Diego,Younis, Yassir,Han, Ze,Bashyam, Sridevi,Zabiulla, Mohammed,Taylor, Dale,Lawrence, Nina,White, Karen L.,Charman, Susan A.,Waterson, David,Witty, Michael J.,Wittlin, Sergio,Botha, Mari?tte E.,Nondaba, Sindisiswe H.,Reader, Janette,Birkholtz, Lyn-Marie,Jiménez-Díaz, María Belén,Martínez, María Santos,Ferrer, Santiago,Angulo-Barturen, Inìigo,Meister, Stephan,Antonova-Koch, Yevgeniya,Winzeler, Elizabeth A.,Street, Leslie J.,Chibale, Kelly
, p. 9890 - 9905 (2016/11/19)
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-2Rnull 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.
