2. Academic Validation
  3. Discovery of boronic acids as novel and potent inhibitors of fatty acid amide hydrolase

Discovery of boronic acids as novel and potent inhibitors of fatty acid amide hydrolase

  • J Med Chem. 2008 Nov 27;51(22):7057-60. doi: 10.1021/jm801051t.
Anna Minkkilä 1,  Susanna M Saario,  Heikki Käsnänen,  Jukka Leppänen,  Antti Poso,  Tapio Nevalainen
Affiliations

Affiliation

  • 1 Department of Pharmaceutical Chemistry, University of Kuopio, P.O. Box 1627, FI-70211 Kuopio, Finland. [email protected]
PMID: 18983140 DOI: 10.1021/jm801051t
Abstract

A series of commercial phenyl-, heteroaryl-, alkyl-, and alkenylboronic acids were evaluated for their FAAH and MGL inhibitory activities. The compounds were generally selective for FAAH, with IC50 in the nanomolar or low-micromolar range. Eight of these compounds inhibited MGL with IC50 in the micromolar range. The most potent compound, phenylboronic acid with para-nonyl substituent (13), inhibited FAAH and MGL with IC50 of 0.0091 and 7.9 microM, respectively.

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