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α-Substituted N-(4-tert-butylbenzyl)-N′-[4-(methylsulfonylamino)benzyl]thiourea analogues as potent and stereospecific TRPV1 antagonists

Title
α-Substituted N-(4-tert-butylbenzyl)-N′-[4-(methylsulfonylamino)benzyl]thiourea analogues as potent and stereospecific TRPV1 antagonists
Authors
Chung J.-U.Kim S.Y.Lim J.-O.Choi H.-K.Kang S.-U.Yoon H.-S.Ryu H.Kang D.W.Lee J.Kang B.Choi S.Toth A.Pearce L.V.Pavlyukovets V.A.Lundberg D.J.Blumberg P.M.
Ewha Authors
최선
SCOPUS Author ID
최선scopus
Issue Date
2007
Journal Title
Bioorganic and Medicinal Chemistry
ISSN
0968-0896JCR Link
Citation
vol. 15, no. 18, pp. 6043 - 6053
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
A series of α-substituted N-(4-tert-butylbenzyl)-N′-[4-(methylsulfonylamino)benzyl]thiourea analogues have been investigated as TRPV1 receptor antagonists. α-Methyl substituted analogues showed potent and stereospecific antagonism to the action of capsaicin on rat TRPV1 heterologously expressed in Chinese hamster ovary cells. In particular, compounds 14 and 18, which possess the R-configuration, exhibited excellent potencies (respectively, K i = 41 and 39.2 nM and K i(ant) = 4.5 and 37 nM). © 2007.
DOI
10.1016/j.bmc.2007.06.041
Appears in Collections:
약학대학 > 약학과 > Journal papers
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