A Positive Charge in an Antimalarial Compound Unlocks Broad-spectrum Antibacterial Activity
Maria Braun-Cornejo,
Mitchell Platteschorre,
Vincent de Vries
et al.
Abstract:In this study, we synthesised a library of eNTRy-rule-complying compounds by introducing ionisable nitrogens to an antimalarial compound. These positively-charged derivatives gained activity against both Gram-negative and -positive bacteria, Mycobacterium tuberculosis and boosted Plasmodium falciparum inhibition to the double-digit nanomolar range. Overcoming and remaining inside the cell envelope of Gram-negative bacteria is one of the major difficulties in antibacterial drug development. The eNTRy rules (N =… Show more
Set email alert for when this publication receives citations?
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.