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Inhibition of monoamine oxidase by indole and benzofuran derivatives.
Eur J Med Chem. 2010 Oct; 45(10):4458-66.EJ

Abstract

Monoamine oxidase (MAO) is an important drug target for the treatment of neurological disorders. A series of indole and benzofuran derivatives were synthesised and evaluated as inhibitors of the two MAO isoforms, MAO-A and MAO-B. In general, the derivatives were found to be selective MAO-B inhibitors with K(i) values in the nanoMolar (nM) to microMolar (microM) concentration range. The most potent MAO-B inhibitor, 3,4-dichloro-N-(2-methyl-1H-indol-5-yl)benzamide, exhibited a K(i) value of 0.03 microM and was 99 fold more selective for the B isoform. We conclude that these indole and benzofuran derivatives are promising reversible MAO-B inhibitors with a possible role in the treatment of neurodegenerative diseases such as Parkinson's disease (PD).

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Authors+Show Affiliations

Prins LH
Pharmaceutical Chemistry, School of Pharmacy, North-West University, Private Bag X6001, Potchefstroom 2520, South Africa.
Petzer JP
No affiliation info available
Malan SF
No affiliation info available

MeSH

BenzofuransHumansIndolesModels, MolecularMonoamine OxidaseMonoamine Oxidase InhibitorsParkinson DiseaseStructure-Activity Relationship

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

20674099

Citation

Prins, Louis H A., et al. "Inhibition of Monoamine Oxidase By Indole and Benzofuran Derivatives." European Journal of Medicinal Chemistry, vol. 45, no. 10, 2010, pp. 4458-66.
Prins LH, Petzer JP, Malan SF. Inhibition of monoamine oxidase by indole and benzofuran derivatives. Eur J Med Chem. 2010;45(10):4458-66.
Prins, L. H., Petzer, J. P., & Malan, S. F. (2010). Inhibition of monoamine oxidase by indole and benzofuran derivatives. European Journal of Medicinal Chemistry, 45(10), 4458-66. https://doi.org/10.1016/j.ejmech.2010.07.005
Prins LH, Petzer JP, Malan SF. Inhibition of Monoamine Oxidase By Indole and Benzofuran Derivatives. Eur J Med Chem. 2010;45(10):4458-66. PubMed PMID: 20674099.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Inhibition of monoamine oxidase by indole and benzofuran derivatives. AU - Prins,Louis H A, AU - Petzer,Jacobus P, AU - Malan,Sarel F, Y1 - 2010/07/31/ PY - 2010/03/10/received PY - 2010/06/08/revised PY - 2010/07/03/accepted PY - 2010/8/3/entrez PY - 2010/8/3/pubmed PY - 2010/12/29/medline SP - 4458 EP - 66 JF - European journal of medicinal chemistry JO - Eur J Med Chem VL - 45 IS - 10 N2 - Monoamine oxidase (MAO) is an important drug target for the treatment of neurological disorders. A series of indole and benzofuran derivatives were synthesised and evaluated as inhibitors of the two MAO isoforms, MAO-A and MAO-B. In general, the derivatives were found to be selective MAO-B inhibitors with K(i) values in the nanoMolar (nM) to microMolar (microM) concentration range. The most potent MAO-B inhibitor, 3,4-dichloro-N-(2-methyl-1H-indol-5-yl)benzamide, exhibited a K(i) value of 0.03 microM and was 99 fold more selective for the B isoform. We conclude that these indole and benzofuran derivatives are promising reversible MAO-B inhibitors with a possible role in the treatment of neurodegenerative diseases such as Parkinson's disease (PD). SN - 1768-3254 UR - https://www.unboundmedicine.com/medline/citation/20674099/Inhibition_of_monoamine_oxidase_by_indole_and_benzofuran_derivatives_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0223-5234(10)00485-X DB - PRIME DP - Unbound Medicine ER -