rdf:type |
|
lifeskim:mentions |
|
pubmed:issue |
5
|
pubmed:dateCreated |
2010-2-22
|
pubmed:abstractText |
We synthesized a series of N(1)-substituted norcymserine derivatives 7a-p and evaluated their anti-cholinesterase activities. In vitro evaluation showed that the pyridinylethyl derivatives 7m-o and the piperidinylethyl derivative 7p improved the anti-butyrylcholinesterase activity by approximately threefold compared to N(1)-phenethylnorcymserine (PEC, 2). A quantitative structure-activity relationship (QSAR) study indicated that logS might be a key feature of the improved compounds.
|
pubmed:language |
eng
|
pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
Mar
|
pubmed:issn |
1464-3405
|
pubmed:author |
pubmed-author:AkaikeAkinoriA,
pubmed-author:FuseShinichiroS,
pubmed-author:HijikuroIchiroI,
pubmed-author:KiharaTakeshiT,
pubmed-author:KunimotoRyoR,
pubmed-author:MurugeshModachur GMG,
pubmed-author:NiidomeTetsuhiroT,
pubmed-author:OkunoYasushiY,
pubmed-author:SugimotoHachiroH,
pubmed-author:TakahashiJunJ,
pubmed-author:TakahashiTakashiT,
pubmed-author:TsumuraYoshinoriY
|
pubmed:copyrightInfo |
Copyright 2010 Elsevier Ltd. All rights reserved.
|
pubmed:issnType |
Electronic
|
pubmed:day |
1
|
pubmed:volume |
20
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
1718-20
|
pubmed:meshHeading |
|
pubmed:year |
2010
|
pubmed:articleTitle |
Design, synthesis, evaluation and QSAR analysis of N(1)-substituted norcymserine derivatives as selective butyrylcholinesterase inhibitors.
|
pubmed:affiliation |
Department of Neuroscience for Drug Discovery, Graduate School of Pharmaceutical Sciences, Kyoto University, 46-29 Yoshida-Shimoadachi-cho, Sakyo-ku, Kyoto 606-8501, Japan.
|
pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
|