Safety of Piperidine-4-carboxamideOn June 1, 2020, Falsini, Matteo; Ceni, Costanza; Catarzi, Daniela; Varano, Flavia; Dal Ben, Diego; Marucci, Gabriella; Buccioni, Michela; Marti Navia, Aleix; Volpini, Rosaria; Colotta, Vittoria published an article in Bioorganic & Medicinal Chemistry Letters. The article was 《New 8-amino-1,2,4-triazolo[4,3-a]pyrazin -3-one derivatives. Evaluation of different moieties on the 6-aryl ring to obtain potent and selective human A2A adenosine receptor antagonists》. The article mentions the following:
In this work, further structural investigations on the 8-amino-2-phenyl-6-aryl-1,2,4-triazolo[4,3-a]pyrazin-3-one series were carried out to achieve potent and selective human A2A adenosine receptor (AR) antagonists. Different ether and amide moieties were attached at the para-position of the 6-Ph ring, thus leading to compounds 1-9 and 10-18, resp. Most of these moieties contained terminal basic rings (pyrrolidine, morpholine, piperidine and substituted piperazines) which were thought to confer good physicochem. and drug-like properties. Compounds 11-16, bearing the amide linker, possessed high affinity and selectivity for the hA2A AR (Ki = 3.6-11.8 nM). Also derivatives 1-9, featuring an ether linker, preferentially targeted the hA2A AR but with lower affinity, compared to those of the relative amide compounds Docking studies, carried out at the hA2A AR binding site, highlighted some crucial ligand-receptor interactions, particularly those provided by the appended substituent whose nature deeply affected hA2A AR affinity. The experimental part of the paper was very detailed, including the reaction process of Piperidine-4-carboxamide(cas: 39546-32-2Safety of Piperidine-4-carboxamide)
Piperidine-4-carboxamide(cas: 39546-32-2) belongs to anime. The methylamines occur in small amounts in some plants. Many polyfunctional amines (i.e., those having other functional groups in the molecule) occur as alkaloids in plants—for example, mescaline, 2-(3,4,5-trimethoxyphenyl)ethylamine; the cyclic amines nicotine, atropine, morphine, and cocaine; and the quaternary salt choline, N-(2-hydroxyethyl)trimethylammonium chloride, which is present in nerve synapses and in plant and animal cells.Safety of Piperidine-4-carboxamide
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem