Novel quinolinepiperazinyl-aryltetrazoles targeting the blood stage of Plasmodium falciparum.

ABSTRACT: The emergence of drug resistance against the frontline antimalarials is a major challenge in the treatment of malaria. In view of emerging reports on drug-resistant strains of Plasmodium against artemisinin combination therapy, a dire need is felt for the discovery of novel compounds acting against novel targets in the parasite. In this study, we identified a novel series of quinolinepiperazinyl-aryltetrazoles (QPTs) targeting the blood stage of Plasmodium. In vitro anti-plasmodial activity screening revealed that most of the compounds showed IC₅₀ < 10 μM against chloroquine-resistant PfINDO strain, with the most promising lead compounds 66 and 75 showing IC₅₀ values of 2.25 and 1.79 μM, respectively. Further, compounds 64-66, 68, 75-77 and

SUBMITTER: Barmade MA 

PROVIDER: S-EPMC10880932 | biostudies-literature | 2024 Feb

REPOSITORIES: biostudies-literature