189442-78-2Relevant articles and documents
Stereoselective Activity of 1-Propargyl-4-styrylpiperidine-like Analogues That Can Discriminate between Monoamine Oxidase Isoforms A and B
Knez, Damijan,Colettis, Natalia,Iacovino, Luca G.,Sova, Matej,Pi?lar, Anja,Konc, Janez,Le?nik, Samo,Higgs, Josefina,Kamecki, Fabiola,Mangialavori, Irene,Dol?ak, Ana,?akelj, Simon,Trontelj, Jurij,Kos, Janko,Binda, Claudia,Marder, Mariel,Gobec, Stanislav
, p. 1361 - 1387 (2020/03/10)
The resurgence of interest in monoamine oxidases (MAOs) has been fueled by recent correlations of this enzymatic activity with cardiovascular, neurological, and oncological 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 analogues selectively target only the MAO-B isoform. The inhibition was studied by kinetic analysis, UV-vis spectrum measurements, and X-ray crystallography. The selective inhibition of the MAO-A and MAO-B isoforms was confirmed ex vivo in mouse brain homogenates, and additional 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.
[1,2,4]-TRIAZOLO [1,5-A]-PYRIMIDINYL DERIVATIVES SUBSTITUTED WITH PIPERIDINE, MORPHOLINE OR PIPERAZINE AS OGA INHIBITORS
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Page/Page column 47; 48, (2018/09/19)
The present invention relates to O-GlcNAc hydrolase (OGA) inhibitors. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which inhibition of OGA is beneficial, such as tauopathies, in particular Alzheimer's disease or progressive supranuclear palsy; and neurodegenerative diseases accompanied by a tau pathology, in particular amyotrophic lateral sclerosis or frontotemporal lobe dementia caused by C90RF72 mutations.
(PIPERIDIN-3-YL)(NAPHTHALEN-2-YL)METHANONE DERIVATIVES AND RELATED COMPOUNDS AS INHIBITORS OF THE HISTONE DEMETHYLASE KDM2B FOR THE TREATMENT OF CANCER
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Page/Page column 130, (2016/08/10)
The present invention relates to (piperidin-3-yl)(naphthalen-2-yl) methanone derivatives and related compounds as inhibitors of one or more histone demethylses, such as KDM2b. The invention also provides pharmaceutically acceptable compositions comprising