828265-69-6Relevant academic research and scientific papers
Design, synthesis and biological evaluation of potential anti-AD hybrids with monoamine oxidase B inhibitory and iron-chelating effects
Guo, Jianan,Mi, Zhisheng,Jiang, Xiaoying,Zhang, Changjun,Guo, Zili,Li, Linzi,Gu, Jinping,Zhou, Tao,Bai, Renren,Xie, Yuanyuan
, (2020/12/29)
A series of active hybrids combining 3-hydroxypyridin-4(1H)-one and coumarin pharmacophores were designed and synthesized as potential agents for the treatment of Alzheimer's disease (AD). All the compounds exhibited excellent iron-chelating activities (p
Chasing ChEs-MAO B Multi-Targeting 4-Aminomethyl-7-Benzyloxy-2H-Chromen-2-ones
Rullo, Mariagrazia,Catto, Marco,Carrieri, Antonio,de Candia, Modesto,Altomare, Cosimo Damiano,Pisani, Leonardo
, (2019/12/25)
A series of 4-aminomethyl-7-benzyloxy-2H-chromen-2-ones was investigated with the aim of identifying multiple inhibitors of cholinesterases (acetyl- and butyryl-, AChE and BChE) and monoamine oxidase B (MAO B) as potential anti-Alzheimer molecules. Starting from a previously reported potent MAO B inhibitor (3), we studied single-point modifications at the benzyloxy or at the basic moiety. The in vitro screening highlighted triple-acting compounds (6, 8, 9, 16, 20) showing nanomolar and selective MAO B inhibition along with IC50 against ChEs at the low micromolar level. Enzyme kinetics analysis toward AChE and docking simulations on the target enzymes were run in order to get insight into the mechanism of action and plausible binding modes.
MAO-B SELECTIVE INHIBITOR COMPOUNDS, PHARMACEUTICAL COMPOSITIONS THEREOF AND USES THEREOF
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Sheet 3, (2015/03/16)
Described herein are a series of compounds having the structure of Formula I for use in the inhibition of MAO and uses thereof for the treatment of a barrier disease, obesity, solid epithelial cell tumor metastasis, diabetes, an auto-immune and inflammatory disease or a cardiometabolic disorder.
Benzouracil-coumarin-arene conjugates as inhibiting agents for chikungunya virus
Hwu, Jih Ru,Kapoor, Mohit,Tsay, Shwu-Chen,Lin, Chun-Cheng,Hwang, Kuo Chu,Horng, Jia-Cherng,Chen, I-Chia,Shieh, Fa-Kuen,Leyssen, Pieter,Neyts, Johan
, p. 103 - 109 (2015/04/22)
Chikungunya virus (CHIKV) is an arbovirus that was first recognized in an epidemic form in East Africa in 1952-1953. The virus is primarily transmitted through mosquitoes and the resulting disease, chikungunya fever, is found in nearly 40 countries. Neith
Discovery of a novel class of potent coumarin monoamine oxidase B inhibitors: Development and biopharmacological profiling of 7-[(3-chlorobenzyl) oxy]-4-[(methylamino)methyl]-2H-chromen-2-one methanesulfonate (NW-1772) as a highly potent, selective, reversible, and orally active monoamine oxidase B inhibitor
Pisani, Leonardo,Muncipinto, Giovanni,Miscioscia, Teresa Fabiola,Nicolotti, Orazio,Leonetti, Francesco,Catto, Marco,Caccia, Carla,Salvati, Patricia,Soto-Otero, Ramon,Mendez-Alvarez, Estefania,Passeleu, Celine,Carotti, Angelo
experimental part, p. 6685 - 6706 (2010/04/04)
In an effort to discover novel selective monoamine oxidase (MAO) B inhibitors with favorable physicochemical and pharmacokinetic profiles, 7-[(m-halogeno)benzyloxy]coumarins bearing properly selected polar substituents at position 4 were designed, synthesized, and evaluated as MAO inhibitors. Several compounds with MAO-B inhibitory activity in the nanomolar range and excellent MAO-B selectivity (selectivity index SI > 400) were identified. Structure-affinity relationships and docking simulations provided valuable insights into the enzyme-inhibitor binding interactions at position 4, which has been poorly explored. Furthermore, computational and experimental studies led to the identification and biopharmacological characterization of 7-[(3-chlorobenzyl)oxy]-4-[(methylamino)-methyl]-2H-chromen-2-one methanesulfonate 22b (NW-1772) as an in vitro and in vivo potent and selective MAO-B inhibitor, with rapid blood-brain barrier penetration, short-acting and reversible inhibitory activity, slight inhibition of selected cytochrome P450s, and low in vitro toxicity. On the basis of this preliminary preclinical profile, inhibitor 22b might be viewed as a promising clinical candidate for the treatment of neurodegenerative diseases.
SUBSTITUTED AMINOALKYL- AND AMIDOALKYL-BENZOPYRAN DERIVATIVES
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Page/Page column 29, (2008/06/13)
This invention is related to novel aminoalkyl- and amidoalkyl- b enzopyran derivatives of the following general formula (I) wherein: the group (a) is a substituent in position 6 or 7 wherein: R is amono- or bi-cyclic (C6-C10) aryl or
Design, synthesis, and 3D QSAR of novel potent and selective aromatase inhibitors
Leonetti, Francesco,Favia, Angelo,Rao, Angela,Aliano, Rosaria,Paluszcak, Anja,Hartmann, Rolf W.,Carotti, Angelo
, p. 6792 - 6803 (2007/10/03)
The design, synthesis, and biological evaluation of a series of new aromatase inhibitors bearing an imidazole or triazole ring linked to a fluorene (A), indenodiazine (B), or coumarin scaffold (C) are reported. Properly substituted coumarin derivatives di
