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6,6-Fused heterocyclic ureas as highly potent TRPV1 antagonists

Title
6,6-Fused heterocyclic ureas as highly potent TRPV1 antagonists
Authors
Sun W.Kim H.-S.Lee S.Jung A.Kim S.-E.Ann J.Yoon S.Choi S.Lee J.H.Blumberg P.M.Frank-Foltyn R.Bahrenberg G.Schiene K.Stockhausen H.Christoph T.Frormann S.Lee J.
Ewha Authors
최선
SCOPUS Author ID
최선scopus
Issue Date
2015
Journal Title
Bioorganic and Medicinal Chemistry Letters
ISSN
0960-894XJCR Link
Citation
vol. 25, no. 4, pp. 803 - 806
Keywords
AnalgesicMolecular modelingTRPV1 antagonistVanilloid receptor 1
Publisher
Elsevier Ltd
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
A series of N-[{2-(4-methylpiperidin-1-yl)-6-(trifluoromethyl)-pyridin-3-yl}methyl] N′-(6,6-fused heterocyclic) ureas have been investigated as hTRPV1 antagonists. Among them, compound 15 showed highly potent TRPV1 antagonism to capsaicin, with Ki(ant) = 0.2 nM, as well as antagonism to other activators, and it was efficacious in a pain model. A docking study of 15 with our hTRPV1 homology model indicates that there is crucial hydrogen bonding between the ring nitrogen and the receptor, contributing to its potency. © 2015 Elsevier Ltd. All rights reserved.
DOI
10.1016/j.bmcl.2014.12.086
Appears in Collections:
약학대학 > 약학과 > Journal papers
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