Li, Ruoxi; Ling, Dazheng; Tang, Tongke; Huang, Zhenghui; Wang, Manjiong; Ding, Yan; Liu, Taiping; Wei, Hanwen; Xu, Wenyue; Mao, Fei; Zhu, Jin; Li, Xiaokang; Jiang, Lubin; Li, Jian published the artcile< Discovery of Novel Plasmodium falciparum HDAC1 Inhibitors with Dual-Stage Antimalarial Potency and Improved Safety Based on the Clinical Anticancer Drug Candidate Quisinostat>, Safety of Ethyl 2-chloropyrimidine-5-carboxylate, the main research area is Plasmodium HDAC HDAC1 inhibitors antimalarials antitumor drug repurposing.
Previously, we identified the clin. anticancer drug candidate quisinostat as a novel and potent antimalarial lead compound To further enhance the antimalarial effect and improve safety, 31 novel spirocyclic hydroxamic acid derivatives were synthesized based on the structure of quisinostat, and their antimalarial activities and cytotoxicity were evaluated. Among them, compound 11 displayed broad potency in vitro against several multi-resistant malarial parasites, especially two artemisinin-resistant clin. isolates. Moreover, 11 could eliminate both liver and erythrocytic parasites in vivo, kill all morphol. erythrocytic parasites with specific potency against schizonts, and show acceptable metabolic stability and pharmacokinetic properties. Western blot anal., PfHDAC gene knockdown, and enzymic inhibition experiments collectively confirmed that PfHDAC1 was the target of 11. In summary, 11 is a structurally novel PfHDAC1 inhibitor with the potential to prevent and cure malaria, overcome multi-drug resistance, and provide a prospective prototype for antimalarial drug research.
Journal of Medicinal Chemistry published new progress about Acetylation (hyperacetylation). 89793-12-4 belongs to class pyrimidines, and the molecular formula is C7H7ClN2O2, Safety of Ethyl 2-chloropyrimidine-5-carboxylate.
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia