| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1358563 | Bioorganic & Medicinal Chemistry Letters | 2016 | 5 Pages |
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.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Enrico Morera, Vincenzo Di Marzo, Ludovica Monti, Marco Allarà, Aniello Schiano Moriello, Marianna Nalli, Giorgio Ortar, Luciano De Petrocellis,