Application of 126832-81-3On March 1, 2008, Imaeda, Yasuhiro; Miyawaki, Toshio; Sakamoto, Hiroki; Itoh, Fumio; Konishi, Noriko; Hiroe, Katsuhiko; Kawamura, Masaki; Tanaka, Toshimasa; Kubo, Keiji published an article in Bioorganic & Medicinal Chemistry. The article was 《Discovery of sulfonylalkylamides: A new class of orally active factor Xa inhibitors》. The article mentions the following:
Factor Xa (FXa) is a trypsin-like serine protease involved in the coagulation cascade and has received great interest as a potential target for the development of new antithrombotic agents. Most of amidine-type FXa inhibitors reported have been found to show extremely poor oral bioavailability. I is one of the first reported non-amidine type FXa inhibitors. To discover novel and orally active FXa inhibitors, we investigated flexible linear linkers between the 6-chloronaphthalene ring and the 1-(pyridin-4-yl)piperidine moiety of I and found an orally active sulfonylalkylamide with an FXa IC50 of 0.05 μM, comparable with that of I. Further modification to reduce the CYP3A4 inhibitory activity of the sulfonylalkylamide resulted in a potent, selective, and orally active 2-methylpyridine analog (FXa IC50 of 0.061 μM), for which the liability of CYP3A4 inhibition was significantly weakened compared to the sulfonylalkylamide. the 2-methylpyridine sulfonylalkylamide analog also showed long lasting anticoagulant activity in cynomolgus monkeys. The experimental part of the paper was very detailed, including the reaction process of 1-Pyridin-4-ylpiperidin-4-one(cas: 126832-81-3Application of 126832-81-3)
1-Pyridin-4-ylpiperidin-4-one(cas: 126832-81-3) belongs to piperidines. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions. Application of 126832-81-3
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem