|
rdf:type |
|
|
lifeskim:mentions |
umls-concept:C0001046,
umls-concept:C0002062,
umls-concept:C0073716,
umls-concept:C0205314,
umls-concept:C0220781,
umls-concept:C0220825,
umls-concept:C0243072,
umls-concept:C0439849,
umls-concept:C0445223,
umls-concept:C0679622,
umls-concept:C1552599,
umls-concept:C1704787,
umls-concept:C1883254
|
|
pubmed:issue |
4
|
|
pubmed:dateCreated |
2010-3-8
|
|
pubmed:abstractText |
A series of novel rutaecarpine derivatives and related alkaloid derivatives 3-aminoalkanamido-substituted rutaecarpine 4a-f and 7,8-dehydrorutaecarpine 5a-c, and 6-aminoalkanamido-substituted 3-[2-(3-Indolyl)ethyl]-4(3a)-quinazolinones 8a-c, were synthesized and subjected to pharmacological evaluation as acetylcholinesterase (AChE) inhibitors. The synthetic compounds exhibited strong inhibitory activity for AChE and high selectivity for AChE over BuChE. The structure-activity relationships were discussed and their binding conformation and simultaneous interactions mode were further clarified by kinetic characterization and the molecular docking studies.
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Apr
|
|
pubmed:issn |
1768-3254
|
|
pubmed:author |
pubmed-author:AnLin-KunLK,
pubmed-author:DingLiL,
pubmed-author:GuLian-QuanLQ,
pubmed-author:HouJin-QiangJQ,
pubmed-author:HuangShi-LiangSL,
pubmed-author:HuangZhi-ShuZS,
pubmed-author:LiYueY,
pubmed-author:MaiYi-ChiYC,
pubmed-author:OuTian-MiaoTM,
pubmed-author:TanJia-HengJH,
pubmed-author:WoodR WRW
|
|
pubmed:copyrightInfo |
Copyright (c) 2009 Elsevier Masson SAS. All rights reserved.
|
|
pubmed:issnType |
Electronic
|
|
pubmed:volume |
45
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
1415-23
|
|
pubmed:meshHeading |
pubmed-meshheading:20079560-Acetylcholinesterase,
pubmed-meshheading:20079560-Alkaloids,
pubmed-meshheading:20079560-Cholinesterase Inhibitors,
pubmed-meshheading:20079560-Drug Evaluation, Preclinical,
pubmed-meshheading:20079560-Indole Alkaloids,
pubmed-meshheading:20079560-Magnetic Resonance Spectroscopy,
pubmed-meshheading:20079560-Models, Molecular,
pubmed-meshheading:20079560-Quinazolines,
pubmed-meshheading:20079560-Spectrometry, Mass, Electrospray Ionization,
pubmed-meshheading:20079560-Structure-Activity Relationship
|
|
pubmed:year |
2010
|
|
pubmed:articleTitle |
Synthesis and evaluation of novel rutaecarpine derivatives and related alkaloids derivatives as selective acetylcholinesterase inhibitors.
|
|
pubmed:affiliation |
School of Pharmaceutical Sciences, Sun Yat-sen University, Waihuan East Road 132, Guangzhou 510006, People's Republic of China.
|
|
pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
|
