Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments.Introducing a new discovery about 388077-74-5, Name is 1-Boc-2-piperidinamide, molecular formula is , belongs to piperidines compound. In a document, author is Szczepanska, Katarzyna, Category: piperidines.
Synthesis and biological activity of novel tert-butyl and tert-pentylphenoxyalkyl piperazine derivatives as histamine H3R ligands
As a continuation of our search for novel histamine H-3 receptor ligands, a series of twenty four new tertbutyl and tert-pentyl phenoxyalkylamine derivatives (2-25) was synthesized. Compounds with three to four carbon atoms alkyl chain spacer were evaluated for their binding properties at human histamine H-3 receptor (hH(3)R). The highest affinities were observed for 4-pyridyl derivatives 4, 10, 16 and 22 (K-i = 16.0 120 nM). As it has been shown in docking studies, those specific heteroaromatic 4-N piperazine substituents might interact with one of the key receptor interacting amino acids. Moreover, the most promising compounds exhibited anticonvulsant activity in the maximal electroshock-induced seizure (MES) model in mice. Furthermore, the blood-brain barrier penetration, the functional H3R antagonist potency as well as the pro-cognitive properties in the passive avoidance test were demonstrated for compound 10. In order to estimate drug-likeness of compound 10, in silico and experimental evaluation of metabolic stability in human liver microsomes was performed. In addition, paying attention to the results obtained within this study, the 4-pyridyl-piperazino moiety has been established as a new bioisosteric piperidine replacement in H3R ligands. (C) 2018 Published by Elsevier Masson SAS.
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Reference:
Piperidine – Wikipedia,
,Piperidine | C5H11N – PubChem