Discovery of a Novel Series of Potent and Selective Alkynylthiazole-Derived PI3Kγ Inhibitors was written by Bandarage, Upul K.;Aronov, Alex M.;Cao, Jingrong;Come, Jon H.;Cottrell, Kevin M.;Davies, Robert J.;Giroux, Simon;Jacobs, Marc;Mahajan, Sudipta;Messersmith, David;Moody, Cameron S.;Swett, Rebecca;Xu, Jinwang. And the article was included in ACS Medicinal Chemistry Letters in 2021.Synthetic Route of C3H9NO The following contents are mentioned in the article:
Phosphoinositide 3-kinases (PI3Ks) are a family of enzymes that control a wide variety of cellular functions such as cell growth, proliferation, differentiation, motility, survival, and intracellular trafficking. PI3Kγ plays a critical role in mediating leukocyte chemotaxis as well as mast cell degranulation, making it a potentially interesting target for autoimmune and inflammatory diseases. We previously disclosed a novel series of PI3Kγ inhibitors derived from a benzothiazole core. The truncation of the benzothiazole core led to the discovery of a structurally diverse alkynyl thiazole series which displayed high PI3Kγ potency and subtype selectivity. Further medicinal chem. optimization of the alkynyl thiazole series led to identification of compounds such as 14 and 32, highly potent, subtype selective, and CNS penetrant PI3Kγ inhibitors. Compound 14 showed robust inhibition of PI3Kγ mediated neutrophil migration in vivo. This study involved multiple reactions and reactants, such as 2-Methoxyethylamine (cas: 109-85-3Synthetic Route of C3H9NO).
2-Methoxyethylamine (cas: 109-85-3) belongs to ethers. Esters typically have a pleasant smell; those of low molecular weight are commonly used as fragrances and are found in essential oils and pheromones. Esterification is the general name for a chemical reaction in which two reactants (typically an alcohol and an acid) form an ester as the reaction product. Esters are common in organic chemistry and biological materials.Synthetic Route of C3H9NO
Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem