|
rdf:type |
|
|
lifeskim:mentions |
|
|
pubmed:issue |
3
|
|
pubmed:dateCreated |
2011-1-24
|
|
pubmed:abstractText |
Optimisation of a screening hit incorporating both TRPV1 activity and solubility was conducted. Substitution of the isoxazole-3-carboxamide with the bespoke 1S, 3R-3-aminocyclohexanol motif afforded the requisite balance of potency and solubility. Compounds 32 and 40 were found to have antihyperalgesic effects in the rat CFA Hg assay and induce a mechanism based hyperthermia.
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Feb
|
|
pubmed:issn |
1464-3405
|
|
pubmed:author |
pubmed-author:AbernethyLynnL,
pubmed-author:AnsariNasrinN,
pubmed-author:CameronKennethK,
pubmed-author:ClarksonTomT,
pubmed-author:DempsterMaureenM,
pubmed-author:DunnDavidD,
pubmed-author:EassonAnna-MarieAM,
pubmed-author:EdwardsDarrenD,
pubmed-author:EverettKatyK,
pubmed-author:FeildenHelenH,
pubmed-author:HoKoc-KanKK,
pubmed-author:KultgenSteveS,
pubmed-author:LittlewoodPeterP,
pubmed-author:MacleanJohnJ,
pubmed-author:McArthurDuncanD,
pubmed-author:McGregorDeborahD,
pubmed-author:McLuskeyHazelH,
pubmed-author:NeaguIrinaI,
pubmed-author:NealeStuartS,
pubmed-author:NisbetLesley-AnneLA,
pubmed-author:OhlmeyerMichaelM,
pubmed-author:PalinRonaldR,
pubmed-author:PhamQuynhchiQ,
pubmed-author:RatcliffePaulP,
pubmed-author:RongYajingY,
pubmed-author:RoughtonAndrewA,
pubmed-author:SammonsMelanieM,
pubmed-author:SwansonRobertR,
pubmed-author:TraceyHeatherH,
pubmed-author:WalkerGlennG
|
|
pubmed:copyrightInfo |
Copyright © 2010 Elsevier Ltd. All rights reserved.
|
|
pubmed:issnType |
Electronic
|
|
pubmed:day |
1
|
|
pubmed:volume |
21
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
892-8
|
|
pubmed:meshHeading |
pubmed-meshheading:21236666-Amides,
pubmed-meshheading:21236666-Animals,
pubmed-meshheading:21236666-Antihypertensive Agents,
pubmed-meshheading:21236666-Cyclohexanols,
pubmed-meshheading:21236666-Hyperthermia, Induced,
pubmed-meshheading:21236666-Isoxazoles,
pubmed-meshheading:21236666-Rats,
pubmed-meshheading:21236666-Rats, Wistar,
pubmed-meshheading:21236666-Structure-Activity Relationship,
pubmed-meshheading:21236666-TRPV Cation Channels
|
|
pubmed:year |
2011
|
|
pubmed:articleTitle |
Structure-activity studies of a novel series of isoxazole-3-carboxamide derivatives as TRPV1 antagonists.
|
|
pubmed:affiliation |
Department of Chemistry, MSD, Newhouse, Lanarkshire, UK. ronnie.palin@gmail.com
|
|
pubmed:publicationType |
Journal Article
|
