A series of 31 arylboronic acids designed on the basis of the pharmacophore model for a variety of TRPV1 antagonists was prepared and tested on FAAH and TRPV1 channel. Four of them, that is, compounds 3c, 4a, 5a,b acted as dual FAAH/TRPV1 blockers with IC50 values between 0.56 and 8.11μM whereas ten others (compounds 1c,f-i, 2c-f, 4b) inhibited FAAH and activated/desensitized TRPV1.
Arylboronic acids as dual-action FAAH and TRPV1 ligands / Morera, Enrico; Di Marzo, Vincenzo; Monti, Ludovica; Allarà, Marco; Schiano Moriello, Aniello; Nalli, Marianna; Ortar, Giorgio; De Petrocellis, Luciano. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - 26:5(2016), pp. 1401-1405. [10.1016/j.bmcl.2016.01.071]
Arylboronic acids as dual-action FAAH and TRPV1 ligands
MORERA, ENRICO
;MONTI, LUDOVICA;NALLI, Marianna;ORTAR, Giorgio;
2016
Abstract
A series of 31 arylboronic acids designed on the basis of the pharmacophore model for a variety of TRPV1 antagonists was prepared and tested on FAAH and TRPV1 channel. Four of them, that is, compounds 3c, 4a, 5a,b acted as dual FAAH/TRPV1 blockers with IC50 values between 0.56 and 8.11μM whereas ten others (compounds 1c,f-i, 2c-f, 4b) inhibited FAAH and activated/desensitized TRPV1.| File | Dimensione | Formato | |
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