Abstract:
BACKGROUND:Due to the complex etiology of neurodegenerative diseases, there is growing interest in multitarget drugs. In this study we synthesized and evaluated a new series of compounds, with benzo[f]coumarin structure, as potential inhibitors of MAO-A, MAO-B, AChE and BuChE. RESULTS:In vitro studies show that most of the studied compounds inhibited the activity of MAO-B in the nano- to micro-molar range. 3-(3´-methoxyphenyl)benzo[f]coumarin is the most active compound with an IC50 value against MAO-B of 2.44 nM. Most of the derivatives exhibited an important selectivity profile against the MAO-B isoform. Some of them also acted as in vitro inhibitors of BuChE, with 3-(2´-hydroxyphenyl)benzo[f]coumarin being the most active with an IC50 value of 1.13 µM. In addition, a theoretical study of the physicochemical properties of the new compounds, as well as a docking study in both MAO isoforms, were carried out. Important structure-activity relationships were obtained. CONCLUSION:Important preliminary structure-activity relationships were concluded from the experimental results. These results encourage us to further explore the potential of this chemical family as potential drug candidates for the treatment of Alzheimer's disease.
journal_name
Future Med Chemjournal_title
Future medicinal chemistryauthors
Matos MJ,Janeiro P,González Franco RM,Vilar S,Tatonetti NP,Santana L,Uriarte E,Borges F,Fontenla JA,Viña Ddoi
10.4155/fmc.14.9subject
Has Abstractpub_date
2014-03-01 00:00:00pages
371-83issue
4eissn
1756-8919issn
1756-8927journal_volume
6pub_type
杂志文章abstract::Chi-Chao Chan, an American board certified ophthalmologist, is the Chief of Immunopathology Section, Laboratory of Immunology and the Head of Histology Core at the National Eye Institute at National Institutes of Health (USA). In 1967, Dr Chan graduated from Chungzhan Medical College in Guangzhou, China and then earne...
journal_title:Future medicinal chemistry
pub_type: 历史文章,面试
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更新日期:2012-11-01 00:00:00
abstract::Filamenting temperature-sensitive mutant Z (FtsZ), an essential cell division protein in bacteria, has recently emerged as an important and exploitable antibacterial target. Cytokinesis in bacteria is regulated by the assembly dynamics of this protein, which is ubiquitously present in eubacteria. The perturbation of F...
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pub_type: 杂志文章,评审
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abstract::Richard H Ebright talks to Rachel Coleby, Commissioning Editor: Ebright is at Rutgers University (New Brunswick, NJ, USA), where he performs research on the structure, mechanism, and regulation of bacterial transcription and on antibacterial drug discovery targeting bacterial transcription. He has received research aw...
journal_title:Future medicinal chemistry
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更新日期:2017-10-01 00:00:00
abstract:AIM:Currently, dozens of BRAF inhibitors and MEK inhibitors targeting RAF-MEK-ERK pathway have been introduced into clinical trials for cancer therapy. However, after 6-8 months of initial response, acquired drug resistance among the majority of those treated patients sharply diminished their clinical efficacy. DISCUS...
journal_title:Future medicinal chemistry
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更新日期:2011-11-01 00:00:00
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journal_title:Future medicinal chemistry
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abstract::Mitochondria play a key role in ATP generation, redox homeostasis and regulation of apoptosis. Due to the essential role of mitochondria in metabolism and cell survival, targeting mitochondria in cancer cells is considered as an attractive therapeutic strategy. However, metabolic flexibility in cancer cells may enable...
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journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
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更新日期:2014-01-01 00:00:00
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pub_type: 杂志文章,评审
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pub_type: 杂志文章
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abstract:BACKGROUND:The objective of this study was to develop and evaluate a more effective mucoadhesive thiomer for buccal drug-delivery systems. METHODS:2-iminothiolane was covalently attached to a chitosan backbone. A preactivation step followed, mediated by 6,6´dithionicotinamide, thiol groups were modified by disulfide b...
journal_title:Future medicinal chemistry
pub_type: 杂志文章
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更新日期:2013-04-01 00:00:00
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pub_type: 杂志文章
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更新日期:2017-12-01 00:00:00
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pub_type: 杂志文章,评审
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更新日期:2013-03-01 00:00:00
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journal_title:Future medicinal chemistry
pub_type: 杂志文章
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更新日期:2009-08-01 00:00:00
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pub_type: 杂志文章,评审
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更新日期:2013-04-01 00:00:00
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journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
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更新日期:2011-06-01 00:00:00
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journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
doi:10.4155/fmc.13.66
更新日期:2013-05-01 00:00:00
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更新日期:2015-01-01 00:00:00
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journal_title:Future medicinal chemistry
pub_type: 杂志文章
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更新日期:2014-02-01 00:00:00
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journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
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更新日期:2019-05-01 00:00:00
abstract:AIM:Due to the complex nature of Alzheimer's disease, there is a renewed search for pleiotropic agents. RESULTS:Purine+coumarin hybrids have been synthesized and tested for the potential treatment of Alzheimer's disease. Hybrids 6, 4a-b, 14c and 14e inhibit significantly soybean lipoxygenase, whereas derivatives 14b, ...
journal_title:Future medicinal chemistry
pub_type: 杂志文章
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pub_type: 杂志文章,评审
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更新日期:2013-12-01 00:00:00
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journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
doi:10.4155/fmc.11.15
更新日期:2011-04-01 00:00:00
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journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
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更新日期:2018-03-01 00:00:00
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journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
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更新日期:2018-01-01 00:00:00
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journal_title:Future medicinal chemistry
pub_type: 杂志文章
doi:10.4155/fmc.09.118
更新日期:2010-02-01 00:00:00
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journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
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更新日期:2016-01-01 00:00:00
abstract::An α-carbonic anhydrases (CAs, EC 4.2.1.1) was recently discovered, cloned and characterized in the genome of the protozoan parasite Trypanosoma cruzi, the causative agent of Chagas disease, a neglected but widespread tropical disease. Inhibition of this α-CAs (TcCA) with anions, sulfonamides, sulfamates, thiols and h...
journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
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更新日期:2016-01-01 00:00:00
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journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
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更新日期:2015-01-01 00:00:00