In 2014,Rzasa, Robert M.; Frohn, Michael J.; Andrews, Kristin L.; Chmait, Samer; Chen, Ning; Clarine, Jeffrey G.; Davis, Carl; Eastwood, Heather A.; Horne, Daniel B.; Hu, Essa; Jones, Adrie D.; Kaller, Matthew R.; Kunz, Roxanne K.; Miller, Silke; Monenschein, Holger; Nguyen, Thomas; Pickrell, Alexander J.; Porter, Amy; Reichelt, Andreas; Zhao, Xiaoning; Treanor, James J. S.; Allen, Jennifer R. published 《Synthesis and preliminary biological evaluation of potent and selective 2-(3-alkoxy-1-azetidinyl) quinolines as novel PDE10A inhibitors with improved solubility》.Bioorganic & Medicinal Chemistry published the findings.Formula: C7H15NO The information in the text is summarized as follows:
We report the discovery of a novel series of 2-(3-alkoxy-1-azetidinyl) quinolines as potent and selective PDE10A inhibitors. Structure-activity studies improved the solubility (pH 7.4) and maintained high PDE10A activity compared to initial lead compound 3, with select compounds demonstrating good oral bioavailability. X-ray crystallog. studies revealed two distinct binding modes to the catalytic site of the PDE10A enzyme. An ex vivo receptor occupancy assay in rats demonstrated that this series of compounds covered the target within the striatum. The experimental part of the paper was very detailed, including the reaction process of 2-(Piperidin-4-yl)ethanol(cas: 622-26-4Formula: C7H15NO)
2-(Piperidin-4-yl)ethanol(cas: 622-26-4) can be used to synthese ursolic acid derivatives, spiroimidazolidinone NPC1L1 inhibitors, neurokinin-2 receptor antagonists, antagonists for inhibition of platelet aggregation.Formula: C7H15NO
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem