Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | 최선 | * |
dc.date.accessioned | 2017-04-25T01:04:28Z | - |
dc.date.available | 2017-04-25T01:04:28Z | - |
dc.date.issued | 2017 | * |
dc.identifier.issn | 0968-0896 | * |
dc.identifier.issn | 1464-3391 | * |
dc.identifier.other | OAK-20425 | * |
dc.identifier.uri | https://dspace.ewha.ac.kr/handle/2015.oak/235014 | - |
dc.description.abstract | A series of 2-substituted 6-t-butylpyridine and 4-t-butylphenyl C-region analogues of 2-(3-fluoro-4-methylsulfonamidophenyl)propanamides were investigated for hTRPV1 antagonism. The analysis of structure activity relationships indicated that the pyridine derivatives generally exhibited a little better antagonism than did the corresponding phenyl surrogates for most of the series. Among the compounds, compound 7 showed excellent antagonism toward capsaicin activation with K-i = 0.1 nM and compound 60S demonstrated a strong antiallodynic effect with 83% MPE at 10 mg/kg in the neuropathic pain model. The docking study of 7S in our hTRPV1 homology model indicated that the interactions between the AFB-regions of 7S with Tyr511 and the interactions between the t-butyl and ethyl groups in the C-region of 7S with the two hydrophobic binding pockets of hTRPV1 contributed to the high potency. (C) 2017 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 | t-Butyl pyridine and phenyl C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent TRPV1 antagonists | * |
dc.type | Article | * |
dc.relation.issue | 8 | * |
dc.relation.volume | 25 | * |
dc.relation.index | SCIE | * |
dc.relation.index | SCOPUS | * |
dc.relation.startpage | 2451 | * |
dc.relation.lastpage | 2462 | * |
dc.relation.journaltitle | BIOORGANIC & MEDICINAL CHEMISTRY | * |
dc.identifier.doi | 10.1016/j.bmc.2017.03.004 | * |
dc.identifier.wosid | WOS:000399437100015 | * |
dc.identifier.scopusid | 2-s2.0-85016300126 | * |
dc.author.google | Lee, Sunho | * |
dc.author.google | Kang, Dong Wook | * |
dc.author.google | Ryu, HyungChul | * |
dc.author.google | Kim, Changhoon | * |
dc.author.google | Ann, Jihyae | * |
dc.author.google | Lee, Hobin | * |
dc.author.google | Kim, Eunhye | * |
dc.author.google | Hong, Sunhye | * |
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 | * |