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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
21
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pubmed:dateCreated |
2010-11-4
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pubmed:abstractText |
We previously proposed that membrane permeabilization activity of NSAIDs is involved in NSAID-induced gastric lesions. We here synthesized derivatives of loxoprofen that have lower membrane permeabilization activity than other NSAIDs. Compared to loxoprofen, the derivatives 10a and 10b have lower membrane permeabilization activity and their oral administration produced fewer gastric lesions but showed an equivalent anti-inflammatory effect. These results suggest that 10a and 10b are likely to be therapeutically beneficial as safer NSAIDs.
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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 |
Nov
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pubmed:issn |
1520-4804
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pubmed:author |
pubmed-author:IshiharaTomoakiT,
pubmed-author:KatsuTakashiT,
pubmed-author:KimotoAyumiA,
pubmed-author:MatoyamaMasaakiM,
pubmed-author:MizushimaTohruT,
pubmed-author:OkamotoYoshinariY,
pubmed-author:OtsukaMasamiM,
pubmed-author:SuemasuShintaroS,
pubmed-author:TakedaMihoM,
pubmed-author:TanakaKen-IchiroK,
pubmed-author:YamakawaNaokiN
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pubmed:issnType |
Electronic
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pubmed:day |
11
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pubmed:volume |
53
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
7879-82
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pubmed:meshHeading |
pubmed-meshheading:20954731-Administration, Oral,
pubmed-meshheading:20954731-Animals,
pubmed-meshheading:20954731-Anti-Inflammatory Agents, Non-Steroidal,
pubmed-meshheading:20954731-Cell Membrane Permeability,
pubmed-meshheading:20954731-Cyclooxygenase Inhibitors,
pubmed-meshheading:20954731-Gastric Mucosa,
pubmed-meshheading:20954731-Gastrointestinal Hemorrhage,
pubmed-meshheading:20954731-Humans,
pubmed-meshheading:20954731-Phenylpropionates,
pubmed-meshheading:20954731-Prodrugs,
pubmed-meshheading:20954731-Rats,
pubmed-meshheading:20954731-Structure-Activity Relationship
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pubmed:year |
2010
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pubmed:articleTitle |
Properties and synthesis of 2-{2-fluoro (or bromo)-4-[(2-oxocyclopentyl)methyl]phenyl}propanoic acid: nonsteroidal anti-inflammatory drugs with low membrane permeabilizing and gastric lesion-producing activities.
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pubmed:affiliation |
Graduate School of Medical and Pharmaceutical Sciences, Kumamoto University, Kumamoto 862-0973, Japan.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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