| pubmed-article:8759636 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:8759636 | lifeskim:mentions | umls-concept:C0003693 | lld:lifeskim |
| pubmed-article:8759636 | lifeskim:mentions | umls-concept:C0040060 | lld:lifeskim |
| pubmed-article:8759636 | lifeskim:mentions | umls-concept:C0038477 | lld:lifeskim |
| pubmed-article:8759636 | lifeskim:mentions | umls-concept:C1321887 | lld:lifeskim |
| pubmed-article:8759636 | lifeskim:mentions | umls-concept:C0243072 | lld:lifeskim |
| pubmed-article:8759636 | pubmed:issue | 16 | lld:pubmed |
| pubmed-article:8759636 | pubmed:dateCreated | 1996-9-24 | lld:pubmed |
| pubmed-article:8759636 | pubmed:abstractText | As part of our research for the development of novel antiinflammatory drug candidates, we have designed and synthesized a series of (E)-3-(1,4-benzoquinonyl)-2-[(3-pyridyl)alkyl]-2-propenoic acid derivatives as dual inhibitors of 5-lipoxygenase (5-LO) and thromboxane (TX) A2 synthetase. In order to increase the absorption after oral administration, we introduced a carboxylic acid moiety into the 1,4-benzoquinone skeleton, which has 5-LO-inhibitory character. Introduction of a 3-pyridylalkyl group at the double bond of the 1,4-benzoquinonyl propenoic acid moiety afforded good to moderate inhibitory activities against the production of leukotriene (LT) B4 and TXA2 while not significantly inhibiting that of prostaglandin E2 by glycogen-induced peritoneal cells of rat (in vitro). The length of the methylene chain of the 3-pyridylalkyl group influenced the inhibition of LTB4 and TXB2 production. An increase of lipophilicity by introducing a more lipophilic alkoxy group did not markedly increase the inhibitory activity on LTB4 production. The position of alkoxy group on the 1,4-benzoquinone skeleton played an important role in TXA2 synthetase inhibition. Compounds such as 20c (E6700) with an appropriate alkoxy group and proper length of methylene side chain, together with a polar substituent (carboxylic acid), showed good inhibition of both 5-LO and TXA2 synthetase and possess a variety of pharmacologically beneficial effects. | lld:pubmed |
| pubmed-article:8759636 | pubmed:language | eng | lld:pubmed |
| pubmed-article:8759636 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:8759636 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:8759636 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:8759636 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:8759636 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:8759636 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
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| pubmed-article:8759636 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:8759636 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:8759636 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:8759636 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:8759636 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:8759636 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:8759636 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:8759636 | pubmed:month | Aug | lld:pubmed |
| pubmed-article:8759636 | pubmed:issn | 0022-2623 | lld:pubmed |
| pubmed-article:8759636 | pubmed:author | pubmed-author:OkamotoYY | lld:pubmed |
| pubmed-article:8759636 | pubmed:author | pubmed-author:MiyamotoKK | lld:pubmed |
| pubmed-article:8759636 | pubmed:author | pubmed-author:KobayashiNN | lld:pubmed |
| pubmed-article:8759636 | pubmed:author | pubmed-author:HaradaKK | lld:pubmed |
| pubmed-article:8759636 | pubmed:author | pubmed-author:KawaharaTT | lld:pubmed |
| pubmed-article:8759636 | pubmed:author | pubmed-author:ShinodaMM | lld:pubmed |
| pubmed-article:8759636 | pubmed:author | pubmed-author:HibiSS | lld:pubmed |
| pubmed-article:8759636 | pubmed:author | pubmed-author:TagamiKK | lld:pubmed |
| pubmed-article:8759636 | pubmed:author | pubmed-author:YamatsuII | lld:pubmed |
| pubmed-article:8759636 | pubmed:author | pubmed-author:NumataHH | lld:pubmed |
| pubmed-article:8759636 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:8759636 | pubmed:day | 2 | lld:pubmed |
| pubmed-article:8759636 | pubmed:volume | 39 | lld:pubmed |
| pubmed-article:8759636 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:8759636 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:8759636 | pubmed:pagination | 3148-57 | lld:pubmed |
| pubmed-article:8759636 | pubmed:dateRevised | 2004-11-17 | lld:pubmed |
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| pubmed-article:8759636 | pubmed:year | 1996 | lld:pubmed |
| pubmed-article:8759636 | pubmed:articleTitle | Structure-activity relationships of (E)-3-(1,4-benzoquinonyl)-2-[(3-pyridyl)-alkyl]-2-propenoic acid derivatives that inhibit both 5-lipoxygenase and thromboxane A2 synthetase. | lld:pubmed |
| pubmed-article:8759636 | pubmed:affiliation | Tsukuba Research Laboratories, Eisai Company Ltd., Ibaraki, Japan. | lld:pubmed |
| pubmed-article:8759636 | pubmed:publicationType | Journal Article | lld:pubmed |
| http://linkedlifedata.com/r... | http://linkedlifedata.com/r... | pubmed-article:8759636 | lld:chembl |
