Arylboronic acids as dual-action FAAH and TRPV1 ligands
Copyright policy )Arylboronic acids as dual-action FAAH and TRPV1 ligands
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.
- National Research Council Italy
- Roma Tre University Italy
- Sapienza University of Rome Italy
- Istituto di Chimica Biomolecolare Italy
Boronic acids, Dose-Response Relationship, Drug, Molecular Structure, boronic acids; dual-ligands; FAAH; fatty acid amide hydrolase; TRPV1; transient receptor potential vanilloid type-1 channel, Dual-ligands, TRPV Cation Channels, Ligands, Boronic Acids, Transient receptor potential vanilloid type-1 channel, Fatty Acid Amide Hydrolases, Amidohydrolases, TRPV1, Inhibitory Concentration 50, Structure-Activity Relationship, Humans, FAAH, Enzyme Inhibitors, Fatty acid amide hydrolase
Boronic acids, Dose-Response Relationship, Drug, Molecular Structure, boronic acids; dual-ligands; FAAH; fatty acid amide hydrolase; TRPV1; transient receptor potential vanilloid type-1 channel, Dual-ligands, TRPV Cation Channels, Ligands, Boronic Acids, Transient receptor potential vanilloid type-1 channel, Fatty Acid Amide Hydrolases, Amidohydrolases, TRPV1, Inhibitory Concentration 50, Structure-Activity Relationship, Humans, FAAH, Enzyme Inhibitors, Fatty acid amide hydrolase
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