Source:http://linkedlifedata.com/resource/pubmed/id/17764957
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
21
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pubmed:dateCreated |
2007-9-17
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pubmed:abstractText |
Acetylcholinesterase reactivators are crucial antidotes for the treatment of organophosphate intoxication. Fifteen new monooxime reactivators of acetylcholinesterase with a (E)-but-2-ene linker were developed in an effort to extend the properties of K-oxime (E)-1-(4-carbamoylpyridinium)-4-(4-hydroxyiminomethylpyridinium)-but-2-ene dibromide (K203). The known reactivators (pralidoxime, HI-6, obidoxime, K075, K203) and the new compounds were tested in vitro on a model of tabun- and paraoxon-inhibited AChE. Monooxime reactivators were not able to exceed the best known compounds for tabun poisoning, but some of them did show reactivation comparable with known compounds for paraoxon poisoning. However, extensive differences were found by a SAR study for various substitutions on the non-oxime part of the reactivator molecule.
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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/Antidotes,
http://linkedlifedata.com/resource/pubmed/chemical/Cholinesterase Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Cholinesterase Reactivators,
http://linkedlifedata.com/resource/pubmed/chemical/Oximes,
http://linkedlifedata.com/resource/pubmed/chemical/Paraoxon,
http://linkedlifedata.com/resource/pubmed/chemical/Phosphoric Acid Esters,
http://linkedlifedata.com/resource/pubmed/chemical/tabun
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pubmed:status |
MEDLINE
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pubmed:month |
Nov
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pubmed:issn |
0968-0896
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
1
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pubmed:volume |
15
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
6733-41
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pubmed:meshHeading |
pubmed-meshheading:17764957-Acetylcholinesterase,
pubmed-meshheading:17764957-Animals,
pubmed-meshheading:17764957-Antidotes,
pubmed-meshheading:17764957-Cholinesterase Inhibitors,
pubmed-meshheading:17764957-Cholinesterase Reactivators,
pubmed-meshheading:17764957-Drug Design,
pubmed-meshheading:17764957-Oximes,
pubmed-meshheading:17764957-Paraoxon,
pubmed-meshheading:17764957-Phosphoric Acid Esters,
pubmed-meshheading:17764957-Rats,
pubmed-meshheading:17764957-Structure-Activity Relationship
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pubmed:year |
2007
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pubmed:articleTitle |
Monooxime reactivators of acetylcholinesterase with (E)-but-2-ene linker: preparation and reactivation of tabun- and paraoxon-inhibited acetylcholinesterase.
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pubmed:affiliation |
Department of Pharmaceutical Chemistry and Drug Control, Faculty of Pharmacy in Hradec Kralove, Charles University in Prague, Heyrovskeho 1203, 500 05, Hradec Kralove, Czech Republic.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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