Discovery and Structure–Activity Relationships of Quinazolinone-2-carboxamide Derivatives as Novel Orally Efficacious Antimalarials
Benoı̂t Laleu, Yuichiro Akao, Atsuko Ochida, Sandra Duffy, Leonardo Lucantoni, David M. Shackleford, Gong Chen, Kasiram Katneni, Francis C. K. Chiu, Karen L. White, Xue Chen, Angelika Sturm, Koen J. Dechering, Benigno Crespo, Laura M. Sanz, Binglin Wang, Sergio Wittlin, Susan A. Charman, Vicky M. Avery, Nobuo Cho, Masahiro Kamaura
Abstract
activity in a murine model of human malaria in a dose-dependent manner constitutes a concomitant benefit.
Topics & Concepts
QuinazolinoneChemistryCarboxamidePharmacologyIn vivoDrug discoveryPlasmodium falciparumStructure–activity relationshipIn vitroPhenotypic screeningMalariaCombinatorial chemistryStereochemistryBiochemistryPhenotypeImmunologyMedicineBiologyGeneBiotechnologyMalaria Research and ControlQuinazolinone synthesis and applicationsHIV/AIDS drug development and treatment