Degorce, Sebastien L. published the artcileImproving metabolic stability and removing aldehyde oxidase liability in a 5-azaquinazoline series of IRAK4 inhibitors, Related Products of pyrimidines, the publication is Bioorganic & Medicinal Chemistry (2020), 28(23), 115815, database is CAplus and MEDLINE.
In this article, we report our efforts towards improving in vitro human clearance in a series of 5-azaquinazolines through a series of C4 truncations and C2 expansions. Extensive DMPK studies enabled us to tackle high Aldehyde Oxidase (AO) metabolism and unexpected discrepancies in human hepatocyte and liver microsomal intrinsic clearance. Our efforts culminated with the discovery of 5-azaquinazoline I, which also displayed exquisite selectivity for IRAK4, and showed synergistic in vitro activity against MyD88/CD79 double mutant ABC-DLBCL in combination with the covalent BTK inhibitor acalabrutinib.
Bioorganic & Medicinal Chemistry published new progress about 1370001-96-9. 1370001-96-9 belongs to pyrimidines, auxiliary class Boronic acid and ester,Boronic acid and ester, name is 4-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyrimidine, and the molecular formula is C11H17BN2O2, Related Products of pyrimidines.
Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/Pyrimidine,
Pyrimidine – Wikipedia