189442-78-2Relevant academic research and scientific papers
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.
Aromatic cycloamines derivative and application in multi-target antidepressant medicine
-
Paragraph 0079; 0080; 0088; 0089; 0104-105, (2019/11/29)
The invention discloses an aromatic cycloamines derivative and an application in multi-target antidepressant medicine. The aromatic cycloamines derivative has inhibitory activity on 5-HT reuptake, NEreuptake and DA reuptake, is a novel compound of a 5-HT/
[1,2,4]-TRIAZOLO [1,5-A]-PYRIMIDINYL DERIVATIVES SUBSTITUTED WITH PIPERIDINE, MORPHOLINE OR PIPERAZINE AS OGA INHIBITORS
-
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.
ARYL-PIPERIDINE DERIVATIVES
-
Paragraph 00338, (2018/10/19)
An aryl-piperidine derivative of formula I, wherein the meaning of R3, X, Cz, and Cy is that specified in the description, for use as inhibitors of T cells.
(PIPERIDIN-3-YL)(NAPHTHALEN-2-YL)METHANONE DERIVATIVES AND RELATED COMPOUNDS AS INHIBITORS OF THE HISTONE DEMETHYLASE KDM2B FOR THE TREATMENT OF CANCER
-
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
NOVEL COMPOUNDS THAT ARE ERK INHIBITORS
-
Page/Page column 80, (2012/05/19)
Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof, wherein: A is a five membered monocyclic heteroaryl ring; and B is a monocyclic heterocycloalkyl ring, or a monocyclic heterocycloalkenyl ring, or a bridge
Identification of small-molecule inhibitors of Trypansoma cruzi replication
Germain, Andrew R.,Carmody, Leigh C.,Dockendorff, Chris,Galan-Rodriguez, Cristina,Rodriguez, Ana,Johnston, Stephen,Bittker, Joshua A.,MacPherson, Lawrence,Dandapani, Sivaraman,Palmer, Michelle,Schreiber, Stuart L.,Munoz, Benito
, p. 7197 - 7200 (2012/01/15)
We report the outcome of a high-throughput small-molecule screen to identify novel, nontoxic, inhibitors of Trypansoma cruzi, as potential starting points for therapeutics to treat for both the acute and chronic stages of Chagas disease. Two compounds wer
NOVEL PROLYLCARBOXYPEPTIDASE INHIBITORS
-
Page/Page column 57, (2011/12/04)
Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.
SUBSTITUTED ARYL SULFONE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS
-
Page/Page column 62, (2010/04/27)
A series of substituted aryl sulfone derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more ot
Hit-to-lead optimization of disubstituted oxadiazoles and tetrazoles as mGluR5 NAMs
Wágner, Gábor,Wéber, Csaba,Nyéki, Olga,Nógrádi, Katalin,Bielik, Attila,Molnár, László,Bobok, Amrita,Horváth, Attila,Kiss, Béla,Kolok, Sándor,Nagy, József,Kurkó, Dalma,Gál, Krisztina,Greiner, István,Szombathelyi, Zsolt,Keser, Gy?rgy M.,Domány, Gy?rgy
scheme or table, p. 3737 - 3741 (2010/08/20)
Here we report the discovery and early SAR of a series of mGluR5 negative allosteric modulators (NAMs). Starting from a moderately active HTS hit we synthesized 3,5-disubstituted-oxadiazoles and tetrazoles as mGluR5 NAMs. Based on the analysis of ligand e
