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Discovery of N-(3-fluoro-4-methylsulfonamidomethylphenyl)urea as a potent TRPV1 antagonistic template

Title
Discovery of N-(3-fluoro-4-methylsulfonamidomethylphenyl)urea as a potent TRPV1 antagonistic template
Authors
Ann, JihyaeSun, WeiZhou, XingJung, AeranBaek, JisooLee, SunhoKim, ChanghoonYoon, SuyoungHong, SunhyeChoi, SunTurcios, Noe A.Herold, Brienna K. A.Esch, Timothy E.Lewin, Nancy E.Abramovitz, AdellePearce, Larry V.Blumberg, Peter M.Lee, Jeewoo
Ewha Authors
최선
SCOPUS Author ID
최선scopus
Issue Date
2016
Journal Title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN
0960-894XJCR Link1464-3405JCR Link
Citation
vol. 26, no. 15, pp. 3603 - 3607
Keywords
Vanilloid receptor 1TRPV1 antagonistsAnalgesic
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
A series of homologous analogues of prototype antagonist 1 and its urea surrogate were investigated as hTRPV1 ligands. Through one-carbon elongation in the respective pharmacophoric regions, N-(3-fluoro-4-methylsulfonamidomethylphenyl)urea was identified as a novel and potent TRPV1 antagonistic template. Its representative compound 27 showed a potency comparable to that of lead compound 1. Docking analysis of compound 27 in our hTRPV1 homology model indicated that its binding mode was similar with that of 1S. (C) 2016 Elsevier Ltd. All rights reserved.
DOI
10.1016/j.bmcl.2016.06.010
Appears in Collections:
약학대학 > 약학과 > Journal papers
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