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
  • 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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