| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1368523 | Bioorganic & Medicinal Chemistry Letters | 2016 | 5 Pages |
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.
Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Jihyae Ann, Wei Sun, Xing Zhou, Aeran Jung, Jisoo Baek, Sunho Lee, Changhoon Kim, Suyoung Yoon, Sunhye Hong, Sun Choi, Noe A. Turcios, Brienna K.A. Herold, Timothy E. Esch, Nancy E. Lewin, Adelle Abramovitz, Larry V. Pearce, Peter M. Blumberg,