Discovery and Structure-Activity Relationships of Quinazolinone-2-carboxamide Derivatives as Novel Orally Efficacious Antimalarials


Journal of Medicinal Chemistry


Laleu, B., Akao, Y., Ochida, A., Duffy, S., Lucantoni, L., Shackleford, D. M., Chen, G., Katneni, K., Chiu, F. C. K., White, K. L., Chen, X., Sturm, A., Dechering, K. J., Crespo, B., Sanz, L. M., Wang, B., Wittlin, S., Charman, S. A., Avery, V. M., … Kamaura, M.



A phenotypic high-throughput screen allowed discovery of quinazolinone-2-carboxamide derivatives as a novel antimalarial scaffold. Structure-activity relationship studies led to identification of a potent inhibitor 19f, 95-fold more potent than the original hit compound, active against laboratory-resistant strains of malaria. Profiling of 19f suggested a fast in vitro killing profile. In vivo activity in a murine model of human malaria in a dose-dependent manner constitutes a concomitant benefit.

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