A series of twenty resveratrol analogues was synthesized and tested on TRPA1 and TRPV1 channels. None was able to significantly modulate TRPV1 channels. Conversely, most of them exhibited remarkably higher TRPA1 modulating activity than resveratrol. Optimal potency was observed with ortho monoxygenated stilbenes 6 and 17.
TRPA1 channels as targets for resveratrol and related stilbenoids / Nalli, Marianna; Ortar, Giorgio; Moriello, Aniello Schiano; Morera, Enrico; Di Marzo, Vincenzo; De Petrocellis, Luciano. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - ELETTRONICO. - 26:3(2016), pp. 899-902. [10.1016/j.bmcl.2015.12.065]
TRPA1 channels as targets for resveratrol and related stilbenoids
NALLI, Marianna
;ORTAR, Giorgio;MORERA, ENRICO;
2016
Abstract
A series of twenty resveratrol analogues was synthesized and tested on TRPA1 and TRPV1 channels. None was able to significantly modulate TRPV1 channels. Conversely, most of them exhibited remarkably higher TRPA1 modulating activity than resveratrol. Optimal potency was observed with ortho monoxygenated stilbenes 6 and 17.| File | Dimensione | Formato | |
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