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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
3
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pubmed:dateCreated |
1994-1-24
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pubmed:abstractText |
Six N-alkyl and N-aryl 5-(1,3,3-trimethylindolinyl) carbamates were synthesized and studied for their structure-activity relationships in inhibiting eel acetylcholinesterase (AChE). The carbamates were 5-(1,3,3-trimethylindolinyl)N,N-dimethylcarbamate (Cui Xing Ning) (I), 5-(1,3,3-trimethylindolinyl)N,N-diethylcarbamate (IV), 5-(1,3,3-trimethylindolinyl)N-ethylcarbamate (III), 5-(1,3,3-trimethylindolinyl)N,N-diethylcarbamate (IV), 5-(1,3,3-trimethylindolinyl)N-heptylcarbamate (V), and 5-(1,3,3-trimethylindolinyl)N-(3-chlorophenyl)carbamate (VI). The inhibition studies were carried out at 25.0 degrees C at pH 7.60. The rank order of the ki values for eel AChE inhibition is II > V > I > III > VI > IV. Compound II has a greater affinity for the enzyme than any irreversible inhibitor cited in the literature (Kd = 7.14 x 10(-8) M). Our findings should aid in the application of these carbamates (1) for counteracting the cholinergic problems associated with various diseases, and (2) for developing potential pretreatment compounds for organophosphate poisoning.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Acetylcholinesterase,
http://linkedlifedata.com/resource/pubmed/chemical/Carbamates,
http://linkedlifedata.com/resource/pubmed/chemical/Cholinesterase Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Indicators and Reagents,
http://linkedlifedata.com/resource/pubmed/chemical/Phosphoric Acid Esters
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pubmed:status |
MEDLINE
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pubmed:issn |
8755-5093
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
5
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
215-23
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:1669449-Acetylcholinesterase,
pubmed-meshheading:1669449-Animals,
pubmed-meshheading:1669449-Carbamates,
pubmed-meshheading:1669449-Cholinesterase Inhibitors,
pubmed-meshheading:1669449-Eels,
pubmed-meshheading:1669449-Indicators and Reagents,
pubmed-meshheading:1669449-Kinetics,
pubmed-meshheading:1669449-Molecular Structure,
pubmed-meshheading:1669449-Phosphoric Acid Esters,
pubmed-meshheading:1669449-Structure-Activity Relationship
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pubmed:year |
1991
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pubmed:articleTitle |
Anticholinesterase activity of potential therapeutic 5-(1,3,3-trimethylindolinyl) carbamates.
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pubmed:affiliation |
U.S. Army Medical Research Institute of Chemical Defense, Aberdeen Proving Ground, Maryland 21010.
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pubmed:publicationType |
Journal Article,
Comparative Study
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