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N-4-t-Butylbenzyl 2-(4-methylsulfonylaminophenyl) propanamide TRPV1 antagonists: Structure-activity relationships in the A-region

Title
N-4-t-Butylbenzyl 2-(4-methylsulfonylaminophenyl) propanamide TRPV1 antagonists: Structure-activity relationships in the A-region
Authors
Kim Y.S.Kil M.-J.Kang S.-U.Ryu H.Kim M.S.Cho Y.Bhondwe R.S.Thorat S.A.Sun W.Liu K.Lee J.H.Choi S.Pearce L.V.Pavlyukovets V.A.Morgan M.A.Tran R.Lazar J.Blumberg P.M.Lee J.
Ewha Authors
최선
SCOPUS Author ID
최선scopus
Issue Date
2012
Journal Title
Bioorganic and Medicinal Chemistry
ISSN
0968-0896JCR Link
Citation
vol. 20, no. 1, pp. 215 - 224
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
Structure-activity relationships for the A-region in a series of N-4-t-butylbenzyl 2-(4-methylsulfonylaminophenyl) propanamides as TRPV1 antagonists have been investigated. Among them, the 3-fluoro analogue 54 showed high binding affinity and potent antagonism for both rTRPV1 and hTRPV1 in CHO cells. Its stereospecific activity was demonstrated with marked selectivity for the (S)-configuration (54S versus 54R). A docking study of 54S with our hTRPV1 homology model highlighted crucial hydrogen bonds between the ligand and the receptor contributing to its potency. © 2011 Elsevier Ltd. All rights reserved.
DOI
10.1016/j.bmc.2011.11.008
Appears in Collections:
약학대학 > 약학과 > Journal papers
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