Piperidine the name comes from the genus name Piper, which is the Latin word for pepper. 84358-13-4, formula is C11H19NO4, Name is 1-(tert-Butoxycarbonyl)piperidine-4-carboxylic acid. Although piperidine is a common organic compound, it is best known as a representative structure element within many pharmaceuticals and alkaloids, such as natural-occurring solenopsins. Synthetic Route of 84358-13-4.
Jung, Young-Hwan;Salmaso, Veronica;Wen, Zhiwei;Bennett, John M.;Phung, Ngan B.;Lieberman, David I.;Gopinatth, Varun;Randle, John C. R.;Chen, Zhoumou;Salvemini, Daniela;Karcz, Tadeusz P.;Cook, Donald N.;Jacobson, Kenneth A. research published 《 Structure-Activity Relationship of Heterocyclic P2Y14 Receptor Antagonists: Removal of the Zwitterionic Character with Piperidine Bioisosteres》, the research content is summarized as follows. A known zwitterionic, heterocyclic P2Y14R antagonist 3a was substituted with diverse groups on the central Ph and terminal piperidine moieties, following a computational selection process. The most potent analogs contained an uncharged piperidine bioisostere, prescreened in silico, while an aza-scan (central Ph ring) reduced P2Y14R affinity. Piperidine amide 11, 3-aminopropynyl 19, and 5-(hydroxymethyl)isoxazol-3-yl) 29 congeners in the triazole series maintained moderate receptor affinity. Adaptation of 5-(hydroxymethyl)isoxazol-3-yl gave the most potent naphthalene-containing (32; MRS4654; IC50, 15 nM) and less active phenylamide-containing (33) scaffolds. Thus, a zwitterion was nonessential for receptor binding, and mol. docking and dynamics probed the hydroxymethylisoxazole interaction with extracellular loops. Also, amidomethyl ester prodrugs were explored to reversibly block the conserved carboxylate group to provide neutral analogs, which were cleavable by liver esterase, and in vivo efficacy demonstrated. We have, in stages, converted zwitterionic antagonists into neutral mols. designed to produce potent P2Y14R antagonists for in vivo application.
84358-13-4, N-BOC-piperidine-4-carboxylic acid, also known asN-Boc-isonipecotic acid , is a useful research compound. Its molecular formula is C11H19NO4 and its molecular weight is 229,28 g/mole. The purity is usually 95%.
N-Boc-isonipecotic acid is a potent antitumor agent that has been clinically shown to be effective against leukemia and lymphoma. It has potent antibacterial activity against Gram-positive bacteria such as Staphylococcus aureus and Streptococcus pyogenes. N-Boc-isonipecotic acid binds to the gyrase enzyme, which is used by these bacteria to maintain the integrity of their DNA, inhibiting protein synthesis and cell division. This drug also has anti-inflammatory properties. N-Boc-isonipecotic acid inhibits prostaglandin synthesis in cells, which may be due to its ability to inhibit the production of tumor necrosis factor α (TNFα) in macrophages., Synthetic Route of 84358-13-4
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem