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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
biochemistry, genetics and molecular biology
Inhibition of monoamine oxidase B by N-methyl-2-phenylmaleimides
Bioorganic and Medicinal Chemistry, Volume 17, No. 8, Year 2009
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Description
Based on a recent report that 1-methyl-3-phenylpyrrolyl analogues are moderately potent reversible inhibitors of the enzyme monoamine oxidase B (MAO-B), a series of structurally related N-methyl-2-phenylmaleimidyl analogues has been prepared and evaluated as inhibitors of MAO-B. In general, the maleimides were more potent competitive inhibitors than the corresponding pyrrolyl analogues. N-Methyl-2-phenylmaleimide was found to be the most potent inhibitor with an enzyme-inhibitor dissociation constant (Ki value) of 3.49 μM, approximately 30-fold more potent than 1-methyl-3-phenylpyrrole (Ki = 118 μM). This difference in activities may be dependent upon the ability of the maleimidyl heterocyclic system to act as a hydrogen bond acceptor. This is in correspondence with literature reports which suggest that hydrogen bond formation is involved in stabilizing inhibitor-MAO-B complexes. Also reported here is a brief kinetic study of the hydrolysis of the N-methyl-2-phenylmaleimidyl analogues in aqueous solution. The findings of the inhibition studies are discussed with reference to the rate and extent of hydrolysis. © 2009 Elsevier Ltd. All rights reserved.
Authors & Co-Authors
Manley-King, Clarina I.
South Africa, Potchefstroom
North-west University
Terre'Blanche, Gisella
South Africa, Potchefstroom
North-west University
Castagnoli, Neal E.
United States, Blacksburg
The Edward Via College of Osteopathic Medicine
Bergh, Jacobus J.
South Africa, Potchefstroom
North-west University
Petzer, Jacobus P.
South Africa, Potchefstroom
North-west University
Statistics
Citations: 20
Authors: 5
Affiliations: 2
Identifiers
Doi:
10.1016/j.bmc.2009.03.005
ISSN:
09680896