Saying a brand new assessment article publication for Acta Materia Medica journal. On this article the authors use medicinal chemistry strategies to establish new chemical entities with larger effectiveness and security than quisinostat.
In whole, 38 novel hydroxamic acid derivatives have been designed and synthesized, and their in vitro antimalarial actions have been systematically investigated. These compounds at nanomolar concentrations confirmed inhibitory results on wild-type and drug-resistant Plasmodium falciparum strains within the erythrocyte stage.
Amongst them, compound 30, after oral administration, resulted in full elimination of parasites in mice contaminated with Plasmodium yoelii, and likewise exhibited higher security and metabolic properties than noticed in our earlier work. Mechanistically, compound 30 upregulated plasmodium histone acetylation, in line with western blotting, thus suggesting that it exerts antimalarial results by means of inhibition of Plasmodium falciparum HDAC enzymes.
Wang, M., et al. (2022) Design and synthesis of novel hydroxamic acid derivatives based mostly on quisinostat as promising antimalarial brokers with improved security. Acta Materia Medica. doi.org/10.15212/AMM-2022-0007.