Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | 최선 | * |
dc.date.accessioned | 2016-08-27T04:08:26Z | - |
dc.date.available | 2016-08-27T04:08:26Z | - |
dc.date.issued | 2015 | * |
dc.identifier.issn | 0968-0896 | * |
dc.identifier.issn | 1464-3391 | * |
dc.identifier.other | OAK-15913 | * |
dc.identifier.uri | https://dspace.ewha.ac.kr/handle/2015.oak/217763 | - |
dc.description.abstract | A series of 2-substituted 4-(trifluoromethyl)benzyl C-region analogs of 2-(3-fluoro-4-methylsulfonamidophenyl)propanamides were investigated for hTRPV1 antagonism. The analysis indicated that the phenyl C-region derivatives exhibited better antagonism than those of the corresponding pyridine surrogates for most of the series examined. Among the phenyl C-region derivatives, the two best compounds 43 and 445 antagonized capsaicin selectively relative to their antagonism of other activators and showed excellent potencies with K-i(CAP) = 0.3 nM. These two compounds blocked capsaicin-induced hypothermia, consistent with TRPV1 as their site of action, and they demonstrated promising analgesic activities in a neuropathic pain model without hyperthermia. The docking study of 445 in our hTRPV1 homology model indicated that its binding mode was similar with that of its pyridine surrogate in the A- and B-regions but displayed a flipped configuration in the C-region. (C) 2015 Elsevier Ltd. All rights reserved. | * |
dc.language | English | * |
dc.publisher | PERGAMON-ELSEVIER SCIENCE LTD | * |
dc.subject | Vanilloid receptor 1 | * |
dc.subject | TRPV1 antagonists | * |
dc.subject | Analgesic | * |
dc.title | Structure activity relationships of benzyl C-region analogs of 2-(3-fluoro-4-methylsulfonamidophenyl)propanamides as potent TRPV1 antagonists | * |
dc.type | Article | * |
dc.relation.issue | 21 | * |
dc.relation.volume | 23 | * |
dc.relation.index | SCI | * |
dc.relation.index | SCIE | * |
dc.relation.index | SCOPUS | * |
dc.relation.startpage | 6844 | * |
dc.relation.lastpage | 6854 | * |
dc.relation.journaltitle | BIOORGANIC & MEDICINAL CHEMISTRY | * |
dc.identifier.doi | 10.1016/j.bmc.2015.10.001 | * |
dc.identifier.wosid | WOS:000364437400007 | * |
dc.identifier.scopusid | 2-s2.0-84946121704 | * |
dc.author.google | Ann, Jihyae | * |
dc.author.google | Jung, Aeran | * |
dc.author.google | Kim, Mi-Yeon | * |
dc.author.google | Kim, Hyuk-Min | * |
dc.author.google | Ryu, HyungChul | * |
dc.author.google | Kim, Sunjoo | * |
dc.author.google | Kang, Dong Wook | * |
dc.author.google | Hong, Sunhye | * |
dc.author.google | Cui, Minghua | * |
dc.author.google | Choi, Sun | * |
dc.author.google | Blumberg, Peter M. | * |
dc.author.google | Frank-Foltyn, Robert | * |
dc.author.google | Bahrenberg, Gregor | * |
dc.author.google | Stockhausen, Hannelore | * |
dc.author.google | Christoph, Thomas | * |
dc.author.google | Lee, Jeewoo | * |
dc.contributor.scopusid | 최선(8659831000) | * |
dc.date.modifydate | 20240305081003 | * |