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.
Keywords:
Boronic acids; Dual-ligands; FAAH; Fatty acid amide hydrolase; TRPV1; Transient receptor potential vanilloid type-1 channel.
Copyright © 2016 Elsevier Ltd. All rights reserved.
MeSH terms
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Amidohydrolases / antagonists & inhibitors*
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Amidohydrolases / metabolism
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Boronic Acids / chemical synthesis
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Boronic Acids / chemistry
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Boronic Acids / pharmacology*
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Dose-Response Relationship, Drug
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology*
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Humans
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Inhibitory Concentration 50
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Ligands
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Molecular Structure
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Structure-Activity Relationship
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TRPV Cation Channels / antagonists & inhibitors*
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TRPV Cation Channels / metabolism
Substances
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Boronic Acids
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Enzyme Inhibitors
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Ligands
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TRPV Cation Channels
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TRPV1 protein, human
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Amidohydrolases
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fatty-acid amide hydrolase