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ID: ALA2086321

Journal: Bioorg Med Chem Lett

Title: Modulation of thermo-transient receptor potential (thermo-TRP) channels by thymol-based compounds.

Authors: Ortar G, Morera L, Moriello AS, Morera E, Nalli M, Di Marzo V, De Petrocellis L.

Abstract: A series of thirty-three thymol, p-cymene-3-carboxylic acid, and 3-amino-p-cymene derivatives was synthesized and tested on TRPA1, TRPM8, and TRPV3 channels. Most of them acted as strong modulators of TRPA1, TRPM8, and TRPV3 channels with EC(50) and/or IC(50) values distinctly lower than those of thymol and related monoterpenoids. Some of the compounds examined, that is, 3c, 4e, f, 6b, and 8b exhibited an appreciable subtype-selectivity.

CiteXplore: 22503249

DOI: 10.1016/j.bmcl.2012.03.055