1. Arylboronic acids as dual-action FAAH and TRPV1 ligands.
- Author
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Morera E, Di Marzo V, Monti L, Allarà M, Schiano Moriello A, Nalli M, Ortar G, and De Petrocellis L
- Subjects
- Amidohydrolases metabolism, Boronic Acids chemical synthesis, Boronic Acids chemistry, Dose-Response Relationship, Drug, Enzyme Inhibitors chemical synthesis, Enzyme Inhibitors chemistry, Humans, Inhibitory Concentration 50, Ligands, Molecular Structure, Structure-Activity Relationship, TRPV Cation Channels metabolism, Amidohydrolases antagonists & inhibitors, Boronic Acids pharmacology, Enzyme Inhibitors pharmacology, TRPV Cation Channels antagonists & inhibitors
- 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., (Copyright © 2016 Elsevier Ltd. All rights reserved.)
- Published
- 2016
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