A novel class of fast-acting antimalarial agents: Substituted 15-membered azalides.

ABSTRACT:

Background and purpose

Efficacy of current antimalarial treatments is declining as a result of increasing antimalarial drug resistance, so new and potent antimalarial drugs are urgently needed. Azithromycin, an azalide antibiotic, was found useful in malaria therapy, but its efficacy in humans is low.

Experimental approach

Four compounds belonging to structurally different azalide classes were tested and their activities compared to azithromycin and chloroquine. in vitro evaluation included testing against sensitive and resistant Plasmodium falciparum, cytotoxicity against HepG2 cells, accumulation and retention in human erythrocytes, antibacterial activity, and mode of action studies (delayed death phenotype and haem polymerization). in vivo assessment enabled determination

SUBMITTER: Peric M 

PROVIDER: S-EPMC9328652 | biostudies-literature | 2021 Jan

REPOSITORIES: biostudies-literature