Valenciano, Ana L.; Ramsey, Aaron C.; Santos, Webster L.; Mackey, Zachary B. published the artcile< Discovery and antiparasitic activity of AZ960 as a Trypanosoma brucei ERK8 inhibitor>, Product Details of C24H15F3N4O, the main research area is AZ960 trypanosomiasis trypanosomicide trypanosoma ERK8 inhibitor; AZ960; Extracellular-signal regulated kinase (ERK); High-throughput screening; Mitogen-activated protein kinase (MAPK); Trypanosoma brucei.
Human African trypanosomiasis (HAT) is a lethal, vector-borne disease caused by the parasite Trypanosoma brucei. Therapeutic strategies for this neglected tropical disease suffer from disadvantages such as toxicity, high cost, and emerging resistance. Therefore, new drugs with novel modes of action are needed. The authors screened cultured T. brucei against a focused kinase inhibitor library to identify promising bioactive compounds Among the ten hits identified from the phenotypic screen, AZ960 I emerged as the most promising compound with potent antiparasitic activity (IC50 = 120 nM) and was shown to be a selective inhibitor of an essential gene product, T. brucei extracellular signal-regulated kinase 8 (TbERK8). The authors report that AZ960 has a Ki of 1.25 μM for TbERK8 and demonstrate its utility in establishing TbERK8 as a potentially druggable target in T. brucei.
Bioorganic & Medicinal Chemistry published new progress about Chagas disease. 1223001-51-1 belongs to class naphthyridine, and the molecular formula is C24H15F3N4O, Product Details of C24H15F3N4O.
Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem