MilliporeSigma
  • 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.

Journal of medicinal chemistry (2008-11-06)
Anna Minkkilä, Susanna M Saario, Heikki Käsnänen, Jukka Leppänen, Antti Poso, Tapio Nevalainen
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.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
4-Methoxyphenylboronic acid, ≥95.0%
Sigma-Aldrich
Phenylboronic acid, 95%
Sigma-Aldrich
4-Biphenylboronic acid, ≥95.0%
Sigma-Aldrich
Benzo[b]thien-2-ylboronic acid, ≥95%
Sigma-Aldrich
3-(Trifluoromethyl)phenylboronic acid, ≥95%