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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 |
2001-5-31
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pubmed:abstractText |
A novel series of indoline derivatives with imidazole and carboxyl moieties were synthesized and evaluated for their thromboxane A2 (TXA2) synthetase inhibiting, radical scavenging and anti-peroxidative activities. Among the compounds synthesized, 3-[5-substituted-3-[2-(imidazol-1-yl)ethyl]indolin-1-yl]propionic acids showed free radical scavenging activity and inhibitory effects on lipid-peroxidation of rat brain homogenate and on arachidonate-induced TXA2-dependent aggregation of rabbit platelets. The anti-platelet and anti-peroxidative activities were related to the lipophilicity of the 5-substituent. The 5-hexyloxy derivative (13) showed about 35-fold higher inhibitory activity on TXA2 synthesis than that of ozagrel and about 100-fold higher activity on lipid peroxidation than that of alpha-tocopherol. Compound 13 showed in vivo anti-thrombotic effect in mice and ex vivo anti-peroxidative activity in rats.
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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 |
0009-2363
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
49
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
563-71
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:11383607-Animals,
pubmed-meshheading:11383607-Arachidonic Acid,
pubmed-meshheading:11383607-Bepridil,
pubmed-meshheading:11383607-Biphenyl Compounds,
pubmed-meshheading:11383607-Blood Platelets,
pubmed-meshheading:11383607-Brain,
pubmed-meshheading:11383607-Chemistry, Physical,
pubmed-meshheading:11383607-Enzyme Inhibitors,
pubmed-meshheading:11383607-Free Radical Scavengers,
pubmed-meshheading:11383607-Indicators and Reagents,
pubmed-meshheading:11383607-Lipid Peroxidation,
pubmed-meshheading:11383607-Magnetic Resonance Spectroscopy,
pubmed-meshheading:11383607-Male,
pubmed-meshheading:11383607-Mice,
pubmed-meshheading:11383607-Physicochemical Phenomena,
pubmed-meshheading:11383607-Picrates,
pubmed-meshheading:11383607-Rabbits,
pubmed-meshheading:11383607-Rats,
pubmed-meshheading:11383607-Rats, Wistar,
pubmed-meshheading:11383607-Spectrophotometry, Infrared,
pubmed-meshheading:11383607-Thromboxane-A Synthase
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pubmed:year |
2001
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pubmed:articleTitle |
A novel series of thromboxane A2 synthetase inhibitors with free radical scavenging and anti-peroxidative activities.
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pubmed:affiliation |
Research Laboratories, Kyoto Pharmaceutical Industries, Ltd., Japan.
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pubmed:publicationType |
Journal Article,
In Vitro
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