Source:http://linkedlifedata.com/resource/pubmed/id/20110173
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
4
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pubmed:dateCreated |
2010-2-17
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pubmed:abstractText |
A series of desloratadine derivatives were stereoselectively synthesized and evaluated for H(1) antihistamine activity. For the evaluation of H(1) antihistamine activity, the in vitro histamine-induced contraction of the guinea-pig ileum assay (HC) was used. The synthesized desloratadine derivatives 7, 8 and 9 are structurally related to rupatadine and were generated by replacement of the 5-methyl-3-pyridine group of rupatadine with gamma-alkylidene butenolide. Their H(1) antihistamine activities have shown a high dependence on the exact nature of the substituent in the lactone ring. Optimum structures 7, 8a and 8g display potent activity inhibiting histamine-induced effects.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Feb
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pubmed:issn |
1464-3391
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pubmed:author | |
pubmed:copyrightInfo |
Copyright 2010 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
18
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1626-32
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pubmed:meshHeading |
pubmed-meshheading:20110173-Animals,
pubmed-meshheading:20110173-Guinea Pigs,
pubmed-meshheading:20110173-Histamine H1 Antagonists, Non-Sedating,
pubmed-meshheading:20110173-Loratadine,
pubmed-meshheading:20110173-Male,
pubmed-meshheading:20110173-Models, Molecular,
pubmed-meshheading:20110173-Spectrometry, Mass, Electrospray Ionization,
pubmed-meshheading:20110173-Spectrophotometry, Infrared,
pubmed-meshheading:20110173-Stereoisomerism
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pubmed:year |
2010
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pubmed:articleTitle |
Stereoselective synthesis of desloratadine derivatives as antagonist of histamine.
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pubmed:affiliation |
School of Pharmaceutical Science, Zhengzhou University, Zhengzhou, PR China.
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pubmed:publicationType |
Journal Article,
In Vitro,
Research Support, Non-U.S. Gov't
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