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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
13
|
pubmed:dateCreated |
1994-8-9
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pubmed:abstractText |
(2RS,4R)-3-(2-(3-Pyridinyl)thiazolidin-4-oyl)indoles represent a new class of potent, orally active antagonists of platelet activating factor (PAF). The compounds were prepared by acylation of the magnesium or zinc salts of substituted indoles with (2RS,4R)-2-(3-pyridinyl)-3-(tert-butoxycarbonyl)thiazolidin-4-oyl chloride. The 3-acylindole moiety functions as a hydrolytically stabilized and conformationally restricted anilide replacement, which imparts a considerable boost in potency to the series. Structure-activity relationships observed for substitution on the indole ring system are discussed. Members of the series compare favorably with other reported PAF antagonists.
|
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical | |
pubmed:status |
MEDLINE
|
pubmed:month |
Jun
|
pubmed:issn |
0022-2623
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pubmed:author | |
pubmed:issnType |
Print
|
pubmed:day |
24
|
pubmed:volume |
37
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
N
|
pubmed:pagination |
2011-32
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:8027984-Administration, Oral,
pubmed-meshheading:8027984-Animals,
pubmed-meshheading:8027984-Capillary Permeability,
pubmed-meshheading:8027984-Edema,
pubmed-meshheading:8027984-Indoles,
pubmed-meshheading:8027984-Magnetic Resonance Spectroscopy,
pubmed-meshheading:8027984-Male,
pubmed-meshheading:8027984-Mice,
pubmed-meshheading:8027984-Platelet Activating Factor,
pubmed-meshheading:8027984-Rabbits,
pubmed-meshheading:8027984-Rats,
pubmed-meshheading:8027984-Rats, Sprague-Dawley,
pubmed-meshheading:8027984-Serotonin,
pubmed-meshheading:8027984-Skin,
pubmed-meshheading:8027984-Stereoisomerism,
pubmed-meshheading:8027984-Structure-Activity Relationship,
pubmed-meshheading:8027984-Thiazoles
|
pubmed:year |
1994
|
pubmed:articleTitle |
3-(2-(3-Pyridinyl)thiazolidin-4-oyl)indoles, a novel series of platelet activating factor antagonists.
|
pubmed:affiliation |
Pharmaceutical Products Division, Abbott Laboratories, Abbott Park, Illinois 60064.
|
pubmed:publicationType |
Journal Article,
Comparative Study,
In Vitro
|