Patel, Snahel; Harris, Seth F.; Gibbons, Paul; Deshmukh, Gauri; Gustafson, Amy; Kellar, Terry; Lin, Han; Liu, Xingrong; Liu, Yanzhou; Liu, Yichin; Ma, Changyou; Scearce-Levie, Kimberly; Ghosh, Arundhati Sengupta; Shin, Young G.; Solanoy, Hilda; Wang, Jian; Wang, Bei; Yin, Jianping; Siu, Michael; Lewcock, Joseph W. published the artcile< Scaffold-Hopping and Structure-Based Discovery of Potent, Selective, And Brain Penetrant N-(1H-Pyrazol-3-yl)pyridin-2-amine Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12)>, Application In Synthesis of 324579-90-0, the main research area is preparation pyrazolylpyridinamine leucine zipper kinase inhibitor.
Recent data suggest that inhibition of dual leucine zipper kinase (DLK, MAP3K12) has therapeutic potential for treatment of a number of indications ranging from acute neuronal injury to chronic neurodegenerative disease. Thus, high demand exists for selective small mol. DLK inhibitors with favorable drug-like properties and good CNS penetration. Herein the authors describe a shape-based scaffold hopping approach to convert pyrimidine 1 to a pyrazole core with improved physicochem. properties. The authors also present the first crystal structures of DLK. By utilizing a combination of property and structure-based design, the authors identified inhibitor I, a potent, selective, and brain-penetrant inhibitor of DLK with activity in an in vivo nerve injury model.
Journal of Medicinal Chemistry published new progress about Blood-brain barrier. 324579-90-0 belongs to class thiazole, and the molecular formula is C6H8N2S, Application In Synthesis of 324579-90-0.
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica