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 8.11 mu M whereas ten others (compounds 1c, f-i, 2c-f, 4b) inhibited FAAH and activated/desensitized TRPV1. (C) 2016 Elsevier Ltd. All rights reserved.
Arylboronic acids as dual-action FAAH and TRPV1 ligands
Di Marzo Vincenzo;De Petrocellis Luciano
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 8.11 mu M whereas ten others (compounds 1c, f-i, 2c-f, 4b) inhibited FAAH and activated/desensitized TRPV1. (C) 2016 Elsevier Ltd. All rights reserved.File in questo prodotto:
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