Cell-based optimization of novel benzamides as potential antimalarial leads

基于细胞的新型苯甲酰胺类化合物优化作为潜在的抗疟先导化合物

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Abstract

Screening our in-house compound collection using a cell based Plasmodium falciparum proliferation assay we discovered a known pan-kinase inhibitor scaffold as a hit. Further optimization of this series led us to a novel benzamide scaffold which was devoid of human kinase activity while retaining its antiplasmodial activity. The evolution of this compound series leading to optimized candidates with good cellular potency against multiple strains as well as decent in vivo profile is described in this Letter.

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