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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
RÉSUMÉ

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