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 EC50 and/or IC50 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. (C) 2012 Elsevier Ltd. All rights reserved.
Modulation of thermo-transient receptor potential (thermo-TRP) channels by thymol-based compounds / Ortar, Giorgio; Morera, Ludovica; Aniello Schiano, Moriello; Morera, Enrico; Nalli, Marianna; Vincenzo Di, Marzo; Luciano De, Petrocellis. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - STAMPA. - 22:10(2012), pp. 3535-3539. [10.1016/j.bmcl.2012.03.055]
Modulation of thermo-transient receptor potential (thermo-TRP) channels by thymol-based compounds
ORTAR, Giorgio;MORERA, LUDOVICA;MORERA, ENRICO;NALLI, Marianna;
2012
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 EC50 and/or IC50 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. (C) 2012 Elsevier Ltd. All rights reserved.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
