Recommanded Product: Piperidine-3-carboxylic acid. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: Piperidine-3-carboxylic acid, is researched, Molecular C6H11NO2, CAS is 498-95-3, about Stereoselective Activity of 1-Propargyl-4-styrylpiperidine-like Analogues That Can Discriminate between Monoamine Oxidase Isoforms A and B. Author is Knez, Damijan; Colettis, Natalia; Iacovino, Luca G.; Sova, Matej; Pislar, Anja; Konc, Janez; Lesnik, Samo; Higgs, Josefina; Kamecki, Fabiola; Mangialavori, Irene; Dolsak, Ana; Zakelj, Simon; Trontelj, Jurij; Kos, Janko; Binda, Claudia; Marder, Mariel; Gobec, Stanislav.
The resurgence of interest in monoamine oxidases (MAOs) has been fueled by recent correlations of this enzymic activity with cardiovascular, neurol., and oncol. disorders. This has promoted increased research into selective MAO-A and MAO-B inhibitors. Here, we shed light on how selective inhibition of MAO-A and MAO-B can be achieved by geometric isomers of cis- and trans-1-propargyl-4-styrylpiperidines. While the cis isomers are potent human MAO-A inhibitors, the trans analogs selectively target only the MAO-B isoform. The inhibition was studied by kinetic anal., UV-vis spectrum measurements, and X-ray crystallog. The selective inhibition of the MAO-A and MAO-B isoforms was confirmed ex vivo in mouse brain homogenates, and addnl. in vivo studies in mice show the therapeutic potential of 1-propargyl-4-styrylpiperidines for central nervous system disorders. This study represents a unique case of stereoselective activity of cis/trans isomers that can discriminate between structurally related enzyme isoforms.
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