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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
5
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pubmed:dateCreated |
2002-3-11
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pubmed:abstractText |
The synthesis and biological activity of novel 1-phenylsulfonyl-4- phenylsulfonylaminopyrrolidine analogues are described. All compounds were produced through modification of the substituent formally corresponding to the 1,3-dioxane ring system and the omega-octenol side chain of thromboxane A(2) (TXA(2)), in reference to the structure of Daltroban. Several compounds were found to be potent TXA(2) receptor antagonists. Compound 51a was the most effective inhibitor of 9,11-epoxymethano PGH(2) (U-46619)-induced rat aortic strip contraction (IC(50)=0.48 nM).
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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 |
0968-0896
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
10
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1399-415
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pubmed:dateRevised |
2004-11-17
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pubmed:meshHeading |
pubmed-meshheading:11886803-15-Hydroxy-11 alpha,9...,
pubmed-meshheading:11886803-Animals,
pubmed-meshheading:11886803-Aorta,
pubmed-meshheading:11886803-Disease Models, Animal,
pubmed-meshheading:11886803-Dogs,
pubmed-meshheading:11886803-Guinea Pigs,
pubmed-meshheading:11886803-Haplorhini,
pubmed-meshheading:11886803-Humans,
pubmed-meshheading:11886803-Male,
pubmed-meshheading:11886803-Mice,
pubmed-meshheading:11886803-Muscle, Smooth, Vascular,
pubmed-meshheading:11886803-Muscle Contraction,
pubmed-meshheading:11886803-Platelet Aggregation,
pubmed-meshheading:11886803-Pulmonary Embolism,
pubmed-meshheading:11886803-Pyrrolidines,
pubmed-meshheading:11886803-Rabbits,
pubmed-meshheading:11886803-Rats,
pubmed-meshheading:11886803-Receptors, Thromboxane,
pubmed-meshheading:11886803-Structure-Activity Relationship,
pubmed-meshheading:11886803-Sulfonamides,
pubmed-meshheading:11886803-Thrombosis,
pubmed-meshheading:11886803-Vasoconstrictor Agents
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pubmed:year |
2002
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pubmed:articleTitle |
Synthesis and biological activity of 1-phenylsulfonyl-4-phenylsulfonylaminopyrrolidine derivatives as thromboxane a(2) receptor antagonists.
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pubmed:affiliation |
Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd. 5-2-3 Tokodai, Tsukuba-shi, 300--2698, Ibaraki, Japan.
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pubmed:publicationType |
Journal Article
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