| pubmed-article:9599246 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:9599246 | lifeskim:mentions | umls-concept:C1419053 | lld:lifeskim |
| pubmed-article:9599246 | lifeskim:mentions | umls-concept:C0076271 | lld:lifeskim |
| pubmed-article:9599246 | lifeskim:mentions | umls-concept:C1289971 | lld:lifeskim |
| pubmed-article:9599246 | lifeskim:mentions | umls-concept:C0231491 | lld:lifeskim |
| pubmed-article:9599246 | lifeskim:mentions | umls-concept:C1554184 | lld:lifeskim |
| pubmed-article:9599246 | lifeskim:mentions | umls-concept:C0675294 | lld:lifeskim |
| pubmed-article:9599246 | pubmed:issue | 11 | lld:pubmed |
| pubmed-article:9599246 | pubmed:dateCreated | 1998-6-15 | lld:pubmed |
| pubmed-article:9599246 | pubmed:abstractText | By incorporating an N-hydroxyurea functionality onto diaryltetrahydrofurans, a novel series of compounds was investigated as dual 5-lipoxygenese (5-LO) inhibitor and platelet-activating factor (PAF) receptor antagonist. These dual functional compounds were evaluated in vitro for 5-LO inhibition in RBL cell extracts and human whole blood, and PAF receptor antagonism in a receptor binding assay. PAF-induced hemoconcentration and arachidonic acid- and TPA-induced ear edema in mice were used to determine in vivo activities. The structure-activity relationship analysis to define a preclinical lead is presented. (+/-)-trans-2-[3-methoxy-4-(4-chlorophenylthioethoxy)-5-(N-methyl- N-h ydroxyureidyl)methylphenyl]-5-(3,4, 5-trimethoxyphenyl)tetrahydrofuran (40, CMI-392) was selected for further study. In the arachidonic acid-induced mouse ear edema model, 40 was more potent than either zileuton (a 5-LO inhibitor) or BN 50739 (a PAF receptor antagonist), and it demonstrated the same inhibitory effect as a physical combination of the latter two agents. These results suggest that a single compound which both inhibits leukotriene synthesis and blocks PAF receptor binding may provide therapeutic advantages over single-acting agents. The clinical development of compound 40 is in progress. | lld:pubmed |
| pubmed-article:9599246 | pubmed:language | eng | lld:pubmed |
| pubmed-article:9599246 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:9599246 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:9599246 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:9599246 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:9599246 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:9599246 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:9599246 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:9599246 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:9599246 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:9599246 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:9599246 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:9599246 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:9599246 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:9599246 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:9599246 | pubmed:month | May | lld:pubmed |
| pubmed-article:9599246 | pubmed:issn | 0022-2623 | lld:pubmed |
| pubmed-article:9599246 | pubmed:author | pubmed-author:HwangS BSB | lld:pubmed |
| pubmed-article:9599246 | pubmed:author | pubmed-author:ShenT YTY | lld:pubmed |
| pubmed-article:9599246 | pubmed:author | pubmed-author:YeeC LCL | lld:pubmed |
| pubmed-article:9599246 | pubmed:author | pubmed-author:CauDD | lld:pubmed |
| pubmed-article:9599246 | pubmed:author | pubmed-author:KillianD BDB | lld:pubmed |
| pubmed-article:9599246 | pubmed:author | pubmed-author:NorMM | lld:pubmed |
| pubmed-article:9599246 | pubmed:author | pubmed-author:QianCC | lld:pubmed |
| pubmed-article:9599246 | pubmed:author | pubmed-author:HussoinM SMS | lld:pubmed |
| pubmed-article:9599246 | pubmed:author | pubmed-author:EckmanJJ | lld:pubmed |
| pubmed-article:9599246 | pubmed:author | pubmed-author:YaegerDD | lld:pubmed |
| pubmed-article:9599246 | pubmed:author | pubmed-author:Libertine-Gar... | lld:pubmed |
| pubmed-article:9599246 | pubmed:author | pubmed-author:ScannellR TRT | lld:pubmed |
| pubmed-article:9599246 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:9599246 | pubmed:day | 21 | lld:pubmed |
| pubmed-article:9599246 | pubmed:volume | 41 | lld:pubmed |
| pubmed-article:9599246 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:9599246 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:9599246 | pubmed:pagination | 1970-9 | lld:pubmed |
| pubmed-article:9599246 | pubmed:dateRevised | 2010-11-18 | lld:pubmed |
| pubmed-article:9599246 | pubmed:meshHeading | pubmed-meshheading:9599246-... | lld:pubmed |
| pubmed-article:9599246 | pubmed:meshHeading | pubmed-meshheading:9599246-... | lld:pubmed |
| pubmed-article:9599246 | pubmed:meshHeading | pubmed-meshheading:9599246-... | lld:pubmed |
| pubmed-article:9599246 | pubmed:meshHeading | pubmed-meshheading:9599246-... | lld:pubmed |
| pubmed-article:9599246 | pubmed:meshHeading | pubmed-meshheading:9599246-... | lld:pubmed |
| pubmed-article:9599246 | pubmed:meshHeading | pubmed-meshheading:9599246-... | lld:pubmed |
| pubmed-article:9599246 | pubmed:meshHeading | pubmed-meshheading:9599246-... | lld:pubmed |
| pubmed-article:9599246 | pubmed:meshHeading | pubmed-meshheading:9599246-... | lld:pubmed |
| pubmed-article:9599246 | pubmed:meshHeading | pubmed-meshheading:9599246-... | lld:pubmed |
| pubmed-article:9599246 | pubmed:meshHeading | pubmed-meshheading:9599246-... | lld:pubmed |
| pubmed-article:9599246 | pubmed:meshHeading | pubmed-meshheading:9599246-... | lld:pubmed |
| pubmed-article:9599246 | pubmed:meshHeading | pubmed-meshheading:9599246-... | lld:pubmed |
| pubmed-article:9599246 | pubmed:meshHeading | pubmed-meshheading:9599246-... | lld:pubmed |
| pubmed-article:9599246 | pubmed:meshHeading | pubmed-meshheading:9599246-... | lld:pubmed |
| pubmed-article:9599246 | pubmed:meshHeading | pubmed-meshheading:9599246-... | lld:pubmed |
| pubmed-article:9599246 | pubmed:meshHeading | pubmed-meshheading:9599246-... | lld:pubmed |
| pubmed-article:9599246 | pubmed:meshHeading | pubmed-meshheading:9599246-... | lld:pubmed |
| pubmed-article:9599246 | pubmed:meshHeading | pubmed-meshheading:9599246-... | lld:pubmed |
| pubmed-article:9599246 | pubmed:meshHeading | pubmed-meshheading:9599246-... | lld:pubmed |
| pubmed-article:9599246 | pubmed:meshHeading | pubmed-meshheading:9599246-... | lld:pubmed |
| pubmed-article:9599246 | pubmed:meshHeading | pubmed-meshheading:9599246-... | lld:pubmed |
| pubmed-article:9599246 | pubmed:meshHeading | pubmed-meshheading:9599246-... | lld:pubmed |
| pubmed-article:9599246 | pubmed:meshHeading | pubmed-meshheading:9599246-... | lld:pubmed |
| pubmed-article:9599246 | pubmed:year | 1998 | lld:pubmed |
| pubmed-article:9599246 | pubmed:articleTitle | (+/-)-trans-2-[3-methoxy-4-(4-chlorophenylthioethoxy)-5-(N-methyl-N- hydroxyureidyl)methylphenyl]-5-(3,4, 5-trimethoxyphenyl)tetrahydrofuran (CMI-392), a potent dual 5-lipoxygenase inhibitor and platelet-activating factor receptor antagonist. | lld:pubmed |
| pubmed-article:9599246 | pubmed:affiliation | CytoMed, Inc., 840 Memorial Drive, Cambridge, Massachusetts 02139, and Department of Chemistry, University of Virginia, Charlottesville, Virginia 22903, USA. | lld:pubmed |
| pubmed-article:9599246 | pubmed:publicationType | Journal Article | lld:pubmed |
| http://linkedlifedata.com/r... | http://linkedlifedata.com/r... | pubmed-article:9599246 | lld:chembl |
