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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
11
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pubmed:dateCreated |
1992-7-8
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pubmed:abstractText |
A class of N-substituted tetrahydrobenzopyrano[3,4-c]pyridines, I, have been identified as antagonists of platelet activating factor (PAF). The structural features essential for PAF binding were determined by systematic modification of three sites in the molecule. While O-alkyl analogues had little effect on binding potency, N-alkyl analogues exhibited a wide range of activity. Structural changes in the core ring system generally resulted in a loss of binding activity. Optimization of the N- and O-substituents resulted in the analogues 25-27 which exhibited Ki values ranging between 131 and 167 nM in a [3H]PAF binding assay. Compound 23 was also active in a model of PAF-induced shock in the mouse following intravenous administration.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
May
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pubmed:issn |
0022-2623
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
29
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pubmed:volume |
35
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2055-61
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:1317924-Alkylation,
pubmed-meshheading:1317924-Animals,
pubmed-meshheading:1317924-Benzopyrans,
pubmed-meshheading:1317924-Bicyclo Compounds,
pubmed-meshheading:1317924-Binding Sites,
pubmed-meshheading:1317924-Blood Platelets,
pubmed-meshheading:1317924-Cell Membrane,
pubmed-meshheading:1317924-Cytoplasmic Granules,
pubmed-meshheading:1317924-Male,
pubmed-meshheading:1317924-Mice,
pubmed-meshheading:1317924-Molecular Structure,
pubmed-meshheading:1317924-Platelet Activating Factor,
pubmed-meshheading:1317924-Platelet Membrane Glycoproteins,
pubmed-meshheading:1317924-Pyridines,
pubmed-meshheading:1317924-Rabbits,
pubmed-meshheading:1317924-Receptors, Cell Surface,
pubmed-meshheading:1317924-Receptors, G-Protein-Coupled,
pubmed-meshheading:1317924-Shock,
pubmed-meshheading:1317924-Structure-Activity Relationship
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pubmed:year |
1992
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pubmed:articleTitle |
Synthesis and structure-activity relationships of a series of novel benzopyran-containing platelet activating factor antagonists.
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pubmed:affiliation |
Immunosciences Research Area, Abbott Laboratories, Abbott Park, Illinois 60064.
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pubmed:publicationType |
Journal Article,
Comparative Study
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