A series of twenty-five derivatives of tetrahydro-beta-carbolines 1-3 was synthesized and assayed on FAAH and TRPV1 and TRPA1 channels. Four carbamates, that is, 5a,c,e, and 9b inhibited FAAH with significant potency and interacted also effectively with TRPV1 and TRPA1 nociceptive receptors, while ureas 7b,d,f, and 8a,b were endowed with specific submicromolar TRPV1 modulating activities. (C) 2012 Elsevier Ltd. All rights reserved.
Tetrahydro-beta-carboline derivatives targeting fatty acid amide hydrolase (FAAH) and transient receptor potential (TRP) channels / Ortar, Giorgio; L., De Petrocellis; A., Schiano Moriello; M., Allara; Morera, Enrico; Nalli, Marianna; V., Di Marzo. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - STAMPA. - 23:1(2013), pp. 138-142. [10.1016/j.bmcl.2012.10.137]
Tetrahydro-beta-carboline derivatives targeting fatty acid amide hydrolase (FAAH) and transient receptor potential (TRP) channels
ORTAR, Giorgio;MORERA, ENRICO;NALLI, Marianna;
2013
Abstract
A series of twenty-five derivatives of tetrahydro-beta-carbolines 1-3 was synthesized and assayed on FAAH and TRPV1 and TRPA1 channels. Four carbamates, that is, 5a,c,e, and 9b inhibited FAAH with significant potency and interacted also effectively with TRPV1 and TRPA1 nociceptive receptors, while ureas 7b,d,f, and 8a,b were endowed with specific submicromolar TRPV1 modulating activities. (C) 2012 Elsevier Ltd. All rights reserved.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
