A5103184623- Malaria Research and Control
- HIV Research and Treatment
- Computational Drug Discovery Methods
- Metal complexes synthesis and properties
- Synthesis and Biological Evaluation
- HIV/AIDS drug development and treatment
University of Pretoria
2022-2025
Mixed-ligand platinum(II) complexes incorporating bipyridine and acyl-thiourea ligands were synthesized evaluated for their in vitro growth inhibitory activity against the human malaria parasite Plasmodium falciparum (Pf). The substituents at four distinct sites varied to identify structure–activity relationships this series. Most displayed potent PfNF54 with IC50 values nanomolar range favorable cytotoxicity profiles. Five (C1, C11, C12, C15, C17) exhibited both asexual blood sexual...
Malaria elimination requires multipronged approaches, including the application of antimalarial drugs able to block human-to-mosquito transmission malaria parasites. The transmissible gametocytes Plasmodium falciparum seem be highly sensitive towards epidrugs, particularly those targeting demethylation histone post-translational marks. Here, we report exploration compounds from a chemical library generated during hit-to-lead optimization inhibitors human lysine demethylase, KDM4B....