Linked Life Data

18072720

Source:http://linkedlifedata.com/resource/pubmed/id/18072720

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SubjectPredicateObjectContext
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pubmed-article:18072720pubmed:abstractTextPreviously, we reported the thiourea antagonists 2a and 2b as potent and high affinity TRPV1 antagonists. For further optimization of the lead compounds, a series of their amide and alpha-substituted amide surrogates were investigated and novel chiral N-(2-benzyl-3-pivaloyloxypropyl) 2-[4-(methylsulfonylamino)phenyl]propionamide analogues were characterized as potent and stereospecific rTRPV1 antagonists. In particular, compounds 72 and 73 displayed high binding affinities, with K i values of 4.12 and 1.83 nM and potent antagonism with K i values of 0.58 and 5.2 nM, respectively, in rTRPV1/CHO cells. These values are comparable or more potent than those of 5-iodoRTX under the same assay conditions. A distinctive binding model that includes two hydrophobic pockets is proposed for this series of compounds based on docking studies of 57 and 72 with a homology model of the TM3/4 region of TRPV1.lld:pubmed
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pubmed-article:18072720pubmed:dateRevised2010-11-18lld:pubmed
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pubmed-article:18072720pubmed:articleTitleStereospecific high-affinity TRPV1 antagonists: chiral N-(2-benzyl-3-pivaloyloxypropyl) 2-[4-(methylsulfonylamino)phenyl]propionamide analogues.lld:pubmed
pubmed-article:18072720pubmed:affiliationResearch Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Shinlim-Dong, Kwanak-Ku, Seoul 151-742, Korea.lld:pubmed
pubmed-article:18072720pubmed:publicationTypeJournal Articlelld:pubmed
pubmed-article:18072720pubmed:publicationTypeResearch Support, Non-U.S. Gov'tlld:pubmed
pubmed-article:18072720pubmed:publicationTypeResearch Support, N.I.H., Intramurallld:pubmed
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