Switch to
Predicate | Object |
---|---|
rdf:type | |
lifeskim:mentions | |
pubmed:issue |
3
|
pubmed:dateCreated |
1997-2-18
|
pubmed:abstractText |
2,5-disubstituted tetrahydrofuran derivatives display a dual functionality: they are PAF antagonists and acetylcholinesterase (AChE) inhibitors. In vitro anti-AChE activity and in vivo trials are presented herein. These compounds are competitive and potent AChE inhibitors. Structure-activity relationships are described and compared with PAF-antagonist results. The presence of an onium group, a suitable distance supplied by a chain of 7 or 10 carbon atoms separating the function from the polar head and an appreciable chain hydrophobicity (4 < sigma f < 7) are the main features required for a dual activity. The derivatives are evaluated in a mouse passive avoidance model. Only compounds with both activities are able to reverse scopolamine-induced amnesia. In addition, they display a very weak toxicity.
|
pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Acetylcholinesterase,
http://linkedlifedata.com/resource/pubmed/chemical/Cholinesterase Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Furans,
http://linkedlifedata.com/resource/pubmed/chemical/Platelet Activating Factor,
http://linkedlifedata.com/resource/pubmed/chemical/tetrahydrofuran
|
pubmed:status |
MEDLINE
|
pubmed:month |
May
|
pubmed:issn |
0929-7855
|
pubmed:author | |
pubmed:issnType |
Print
|
pubmed:volume |
13
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
207-22
|
pubmed:dateRevised |
2006-11-15
|
pubmed:meshHeading |
pubmed-meshheading:8816985-Acetylcholinesterase,
pubmed-meshheading:8816985-Adult,
pubmed-meshheading:8816985-Animals,
pubmed-meshheading:8816985-Cholinesterase Inhibitors,
pubmed-meshheading:8816985-Furans,
pubmed-meshheading:8816985-Humans,
pubmed-meshheading:8816985-Male,
pubmed-meshheading:8816985-Mice,
pubmed-meshheading:8816985-Mice, Inbred C57BL,
pubmed-meshheading:8816985-Platelet Activating Factor,
pubmed-meshheading:8816985-Structure-Activity Relationship
|
pubmed:year |
1996
|
pubmed:articleTitle |
Structure-activity relationships in platelet-activating factor (PAF). 8. Tetrahydrofuran derivatives as dual PAF antagonists and acetylcholinesterase inhibitors: anti-acetylcholinesterase activity and comparative SAR.
|
pubmed:affiliation |
Université Paris 7-Denis Diderot, France.
|
pubmed:publicationType |
Journal Article,
Comparative Study
|