Synthesis and structure-activity relationship of disubstituted benzamides as a novel class of antimalarial agents

Katsuhiko Mitachi; Yandira G Salinas; Michele Connelly; Nicholas Jensen; Taotao Ling; Fatima Rivas

doi:10.1016/j.bmcl.2012.05.124

Synthesis and structure-activity relationship of disubstituted benzamides as a novel class of antimalarial agents

Bioorg Med Chem Lett. 2012 Jul 15;22(14):4536-9. doi: 10.1016/j.bmcl.2012.05.124. Epub 2012 Jun 7.

Authors

Katsuhiko Mitachi¹, Yandira G Salinas, Michele Connelly, Nicholas Jensen, Taotao Ling, Fatima Rivas

Affiliation

¹ Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, 262 Danny Thomas Place, Memphis, TN 38105-3678, USA.

PMID: 22727641
DOI: 10.1016/j.bmcl.2012.05.124

Abstract

Malaria is a devastating world health problem. Using a compound library screening approach, we identified a novel series of disubstituted benzamide compounds with significant activity against malaria strains 3D7 and K1. These compounds represent a new antimalarial molecular scaffold exemplified by compound 1, which demonstrated EC(50) values of 60 and 430 nM against strains 3D7 and K1, respectively. Herein we report our findings on the efficient synthesis, structure-activity relationships, and biological activity of this new class of antimalarial agents.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Antimalarials / chemical synthesis*
Antimalarials / pharmacology
Benzamides / chemical synthesis*
Benzamides / pharmacology
Cell Line
Humans
Molecular Structure
Plasmodium falciparum / drug effects
Structure-Activity Relationship

Substances

Antimalarials
Benzamides