Related Products of 233276-38-5. Let¡¯s face it, organic chemistry can seem difficult to learn. Especially from a beginner¡¯s point of view. Like 233276-38-5, Name is 4-Methyltetrahydro-2H-pyran-4-carboxylic acid. In a document type is Article, introducing its new discovery.
Discovery and biological evaluation of novel pyrazolopyridine derivatives as potent and orally available PI3Kdelta inhibitors
Phosphatidylinositol-3-kinase (PI3K)delta inhibition is one of the most attractive approaches to the treatment of autoimmune diseases and leukocyte malignancies. Through the exploration of pyrazolopyridine derivatives as potential PI3Kdelta inhibitors, compound 12a was identified as a potent PI3Kdelta inhibitor but suffered from poor oral exposure in mice. With a modified amide linkage group, compound 15a was developed as an orally available PI3Kdelta inhibitor with reduced selectivity against other PI3Ks. To improve the trade-off between selectivity and PK profile, structure?activity relationship (SAR) studies of terminal substituents on the pyrolidine ring were conducted. As a result, we developed potent PI3Kdelta inhibitors with good oral availability. In particular, the representative compound 15j showed excellent selectivity for PI3Kdelta over other PI3Ks with good oral exposure in mice.
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Reference£º
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics