Journal article
Arylboronic acids as dual-action FAAH and TRPV1 ligands
E Morera, V Di Marzo, L Monti, M Allarà, A Schiano Moriello, M Nalli, G Ortar, L De Petrocellis
Bioorganic and Medicinal Chemistry Letters | Published : 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 μM whereas ten others (compounds 1c,f-i, 2c-f, 4b) inhibited FAAH and activated/desensitized TRPV1.
Grants
Awarded by Sapienza Università di Roma
Funding Acknowledgements
This research was supported by Sapienza Universita di Roma (Grant No C26A14TLFT).