| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1367077 | Bioorganic & Medicinal Chemistry Letters | 2007 | 4 Pages |
Abstract
Starting from ROPA (2), analogues of RTX (1a) modified on the acyl side chain were prepared and evaluated for vanilloid activity in HEK-293 cells over-expressing the human recombinant TRPV1. The ROPA motif provided an enhancement of potency sufficient to expand the range of vanillyl surrogates to structural elements (e.g., an unsubstituted phenyl ring) that afford inactive analogues in compounds from the capsaicin series.
Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Giovanni Appendino, Abdellah Ech-Chahad, Alberto Minassi, Sara Bacchiega, Luciano De Petrocellis, Vincenzo Di Marzo,