Discovery and Characterization of Selective and Ligand-Efficient DYRK Inhibitors was written by Henderson, Scott H.;Sorrell, Fiona;Bennett, James;Fedorov, Oleg;Hanley, Marcus T.;Godoi, Paulo H.;Ruela de Sousa, Roberta;Robinson, Sean;Ashall-Kelly, Alexander;Hopkins Navratilova, Iva;Walter, Daryl S.;Elkins, Jonathan M.;Ward, Simon E.. And the article was included in Journal of Medicinal Chemistry in 2021.Synthetic Route of C5H6N2O This article mentions the following:
Dual-specificity tyrosine-regulated kinase 1A (DYRK1A) regulates the proliferation and differentiation of neuronal progenitor cells during brain development. Consequently, DYRK1A has attracted interest as a target for the treatment of neurodegenerative diseases, including Alzheimer’s disease (AD) and Down’s syndrome. Recently, the inhibition of DYRK1A has been investigated as a potential treatment for diabetes, while DYRK1A’s role as a mediator in the cell cycle has garnered interest in oncol. indications. Structure-activity relationship (SAR) anal. in combination with high-resolution X-ray crystallog. leads to a series of pyrazolo[1,5-b]pyridazine inhibitors with excellent ligand efficiencies, good physicochem. properties, and a high degree of selectivity over the kinome. Compound 11 (I) exhibited good permeability and cellular activity without P-glycoprotein liability, extending the utility of 11 in an in vivo setting. These pyrazolo[1,5-b]pyridazines are a viable lead series in the discovery of new therapies for the treatment of diseases linked to DYRK1A function. In the experiment, the researchers used many compounds, for example, 3-Methoxypyridazine (cas: 19064-65-4Synthetic Route of C5H6N2O).
3-Methoxypyridazine (cas: 19064-65-4) belongs to pyridazine derivatives. The pyridazine structure is a popular pharmacophore which is found within a number of herbicides such as credazine, pyridafol and pyridate. In the past decade, X-ray data were reported with regard to the characterization and structural elucidation of a number of pyridazine-metal complexes, including pyridazine ligands with zinc, nickel, copper, cadmium and ruthenium.Synthetic Route of C5H6N2O
Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem