1360874-99-2Relevant academic research and scientific papers
Synthesis and biological evaluation of [6]-gingerol analogues as transient receptor potential channel TRPV1 and TRPA1 modulators
Morera, Enrico,De Petrocellis, Luciano,Morera, Ludovica,Moriello, Aniello Schiano,Nalli, Marianna,Di Marzo, Vincenzo,Ortar, Giorgio
, p. 1674 - 1677 (2012)
In order to explore the structural determinants for the TRPV1 and TRPA1 agonist properties of gingerols, aseries 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). 2011 Elsevier Ltd. All rights reserved.
