N-Acylethanolamine acid amidase (NAAA) inhibitors found to enhance palmitoylethanolamide levels

Schermafbeelding 2013-12-05 om 23.21.54

The scientific group of professor D. Piomelli (USA) looks for new ways to enhance palmitoylethanolamide in cells. To help these cells against injury. In their recent article:

Synthesis, Structure-Activity, and Structure-Stability Relationships of 2-Substituted-N-(4-oxo-3-oxetanyl) N-Acylethanolamine Acid Amidase (NAAA) Inhibitors

they described new molecules of class of α-amino-β-lactones as new important and selective NAAA inhibitor. These molecules have been shown to have a clear anti-inflammatory effects. These effects are mediated through palmitoylethanolamide- activation of PPAR-α.

It will however take 10 more years before any of these molecules will enter the clinic, if ever. In the mean time the substitution with palmitoylethanolamide is proven to be the best way to supply the body with this protective molecule. Dose recommendation as a starting dose: 3 times 400 mg/daily.

Source:
Vitale R, Ottonello G, Petracca R, Bertozzi SM, Ponzano S, Armirotti A, Berteotti A, Dionisi M, Cavalli A, Piomelli D, Bandiera T, Bertozzi F. Synthesis, Structure-Activity, and Structure-Stability Relationships of 2-Substituted-N-(4-oxo-3-oxetanyl) N-Acylethanolamine Acid Amidase (NAAA) Inhibitors.
ChemMedChem. 2014 Jan 8. doi: 10.1002/cmdc.201300416.

Leave a Reply

Fill in your details below or click an icon to log in:

WordPress.com Logo

You are commenting using your WordPress.com account. Log Out / Change )

Twitter picture

You are commenting using your Twitter account. Log Out / Change )

Facebook photo

You are commenting using your Facebook account. Log Out / Change )

Google+ photo

You are commenting using your Google+ account. Log Out / Change )

Connecting to %s

%d bloggers like this: