☆ 4.5 Article

Selected furanochalcones as inhibitors of monoamine oxidase

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2013)

期刊

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷 23, 期 17, 页码 4985-4989

出版社

PERGAMON-ELSEVIER SCIENCE LTD

DOI: 10.1016/j.bmcl.2013.06.050

关键词

Chalcone; Monoamine oxidase; MAO-B; Reversible inhibition; Competitive

类别

Chemistry, Medicinal Chemistry, Organic

资金

North-West University
National Research Foundation (NRF)
Medical Research Council (MRC), South Africa

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Reagent

摘要

The validity of the chalcone scaffold for the design of inhibitors of monoamine oxidase has previously been illustrated. In a systematic attempt to investigate the effect of heterocyclic substitution on the monoamine oxidase inhibitory properties of this versatile scaffold, a series of furanochalcones were synthesized. The results demonstrate that these furan substituted phenylpropenones exhibited moderate to good inhibitory activities towards MAO-B, but showed weak or no inhibition of the MAO-A enzyme. The most active compound, 2E-3-(5-chlorofuran-2-yl)-1-(3-chlorophenyl)prop-2-en-1-one, exhibited an IC50 value of 0.174 mu M for the inhibition of MAO-B and 28.6 mu M for the inhibition of MAO-A. Interestingly, contrary to data previously reported for chalcones, these furan substituted derivatives acted as reversible inhibitors, while kinetic analysis revealed a competitive mode of binding. (C) 2013 Elsevier Ltd. All rights reserved.

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