2. Academic Validation
  3. Design, synthesis and biological evaluation of potent FAAH inhibitors

Design, synthesis and biological evaluation of potent FAAH inhibitors

  • Bioorg Med Chem Lett. 2016 Jun 1;26(11):2701-5. doi: 10.1016/j.bmcl.2016.04.004.
Wei Tuo 1,  Natascha Leleu-Chavain 1,  Amélie Barczyk 1,  Nicolas Renault 1,  Lucas Lemaire 1,  Philippe Chavatte 1,  Régis Millet 2
Affiliations

Affiliations

  • 1 ICPAL, Univ. Lille, Inserm, U995-LIRIC-Lille Inflammation Research International Center, 3 rue du Professeur Laguesse BP83, F-59006 Lille, France.
  • 2 ICPAL, Univ. Lille, Inserm, U995-LIRIC-Lille Inflammation Research International Center, 3 rue du Professeur Laguesse BP83, F-59006 Lille, France. Electronic address: regis.millet@univ-lille2.fr.
PMID: 27117424 DOI: 10.1016/j.bmcl.2016.04.004
Abstract

A new series of 3-carboxamido-5-aryl-isoxazoles was designed, synthesized and evaluated for their biological activity. Different pharmacomodulations have been explored and the lipophilicity of these compounds was assessed. Investigation of the in vitro biological activity led to the identification of 5 compounds as potent FAAH inhibitors, their good FAAH inhibition capacity is probably correlated with their suitable lipophilicity. Specifically, compound 25 showed similar inhibition potency against FAAH in comparison with URB597, one of the most potent FAAH Inhibitor known to date.

Keywords

AEA; Cannabinoid receptors; FAAH inhibitor; PEA; PPAR-α.

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