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Discovery of N-(3-fluoro-4-methylsulfonamidomethylphenyl)urea as a potent TRPV1 antagonistic template.
- Source :
-
Bioorganic & Medicinal Chemistry Letters . Aug2016, Vol. 26 Issue 15, p3603-3607. 5p. - Publication Year :
- 2016
-
Abstract
- A series of homologous analogues of prototype antagonist 1 and its urea surrogate were investigated as h TRPV1 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 h TRPV1 homology model indicated that its binding mode was similar with that of 1 S . [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 0960894X
- Volume :
- 26
- Issue :
- 15
- Database :
- Academic Search Index
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Publication Type :
- Academic Journal
- Accession number :
- 116843593
- Full Text :
- https://doi.org/10.1016/j.bmcl.2016.06.010