Journal of medicinal and pharmaceutical chemistry 2008-11-27

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

Anna Minkkilä, Susanna M Saario, Heikki Käsnänen, Jukka Leppänen, Antti Poso, Tapio Nevalainen

Index: J. Med. Chem. 51 , 7057-7060, (2008)

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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.