Bryan, Marian C. published the artcileDevelopment of Potent and Selective Pyrazolopyrimidine IRAK4 Inhibitors, Application of Piperidine-4-carboxamide, the publication is Journal of Medicinal Chemistry (2019), 62(13), 6223-6240, database is CAplus and MEDLINE.
A series of pyrazolopyrimidine inhibitors of IRAK4 were developed from a high-throughput screen (HTS). Modification of an HTS hit led to a series of bicyclic heterocycles with improved potency and kinase selectivity but lacking sufficient solubility to progress in vivo. Structure-based drug design, informed by cocrystal structures with the protein and small-mol. crystal structures, yielded a series of dihydrobenzofurans. This semisatd. bicycle provided superior druglike properties while maintaining excellent potency and selectivity. Improved physicochem. properties allowed for progression into in vivo experiments, where lead mols. exhibited low clearance and showed target-based inhibition of IRAK4 signaling in an inflammation-mediated PK/PD mouse model.
Journal of Medicinal Chemistry published new progress about 39546-32-2. 39546-32-2 belongs to piperidines, auxiliary class Piperidine,Amine,Amide, name is Piperidine-4-carboxamide, and the molecular formula is C6H12N2O, Application of Piperidine-4-carboxamide.
Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem