Discovery and Structure-Activity Relationships of Quinazolinone-2-carboxamide Derivatives as Novel Orally Efficacious Antimalarials
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Akao, Yuichiro
Ochida, Atsuko
Duffy, Sandra
Lucantoni, Leonardo
Shackleford, David M
Chen, Gong
Katneni, Kasiram
Chiu, Francis CK
White, Karen L
Chen, Xue
Sturm, Angelika
Dechering, Koen J
Avery, Vicky M
et al.
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Abstract
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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Journal of Medicinal Chemistry
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© The Author(s) 2021. This is an Open Access article distributed under the terms of the Creative Commons Attribution-NonCommercial-NoDerivs 4.0 International (CC BY-NC-ND 4.0) License, which permits unrestricted, non-commercial use, distribution and reproduction in any medium, providing that the work is properly cited.
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Macromolecular and materials chemistry
Organic chemistry
Pharmacology and pharmaceutical sciences
Medicinal and biomolecular chemistry
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Laleu, B; Akao, Y; Ochida, A; Duffy, S; Lucantoni, L; Shackleford, DM; Chen, G; Katneni, K; Chiu, FCK; White, KL; Chen, X; Sturm, A; Dechering, KJ; Avery, VMet al., Discovery and Structure-Activity Relationships of Quinazolinone-2-carboxamide Derivatives as Novel Orally Efficacious Antimalarials, Journal of Medicinal Chemistry, 2021