The Multistage Antimalarial Compound Calxinin Perturbates P. falciparum Ca²⁺ Homeostasis by Targeting a Unique Ion Channel.

ABSTRACT: Malaria elimination urgently needs novel antimalarial therapies that transcend resistance, toxicity, and high costs. Our multicentric international collaborative team focuses on developing multistage antimalarials that exhibit novel mechanisms of action. Here, we describe the design, synthesis, and evaluation of a novel multistage antimalarial compound, 'Calxinin'. A compound that consists of hydroxyethylamine (HEA) and trifluoromethyl-benzyl-piperazine. Calxinin exhibits potent inhibitory activity in the nanomolar range against the asexual blood stages of drug-sensitive (3D7), multidrug-resistant (Dd2), artemisinin-resistant (IPC4912), and fresh Kenyan field isolated Plasmodium falciparum strains. Calxinin treatment resulted in diminished maturation of parasite sexual precursor cel

SUBMITTER: Gupta Y 

PROVIDER: S-EPMC9319510 | biostudies-literature | 2022 Jun

REPOSITORIES: biostudies-literature