Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1371799 | Bioorganic & Medicinal Chemistry Letters | 2012 | 4 Pages |
Abstract
In order to explore the structural determinants for the TRPV1 and TRPA1 agonist properties of gingerols, a series of nineteen analogues (1b–5) of racemic [6]-gingerol (1a) was synthesized and tested on TRPV1 and TRPA1 channels. The exploration of the structure–activity relationships, by modulating the three pharmacophoric regions of [6]-gingerol, led to the identification of some selective TRPV1 agonists/desensitizers of TRPV1 channels (3a, 3f, and 4) and of some full TRPA1 antagonists (2c, 2d, 3b, and 3d).
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Enrico Morera, Luciano De Petrocellis, Ludovica Morera, Aniello Schiano Moriello, Marianna Nalli, Vincenzo Di Marzo, Giorgio Ortar,