期刊
MOLECULAR DIVERSITY
卷 24, 期 2, 页码 391-406出版社
SPRINGER
DOI: 10.1007/s11030-019-09960-5
关键词
Monoamine oxidase; MAO; Inhibition; Reversible; Quinazolinone; Neurodegenerative disorders
类别
资金
- National Research Foundation
- Medical Research Council of South Africa [85642, 96180, 916135]
Quinazolinone compounds are of interest in medicinal chemistry since they display a wide range of biological properties. In the present study, a series of C6- and N1-substituted 3-methyl-3,4-dihydroquinazolin-2(1H)-one derivatives were synthesised and evaluated as inhibitors of recombinant human monoamine oxidase (MAO). Some of these quinazolinones are structurally related to a series of 3,4-dihydro-2(1H)-quinolinone derivatives, which have previously been reported to act as specific inhibitors of MAO-B. The results document that, among 37 compounds synthesised, seven displayed IC50 values < 1 mu M for the inhibition of MAO-B. The most potent MAO-A inhibitor exhibits an IC50 value of 7.43 mu M while the most potent MAO-B inhibitor possesses an IC50 value of 0.269 mu M. Good-potency MAO inhibition was only observed among C6-substituted 3-methyl-3,4-dihydroquinazolin-2(1H)-one derivatives with N1-substitution yielding comparatively low-potency inhibition. MAO-B-specific inhibitors such as some of the quinazolinone compounds investigated here may act as leads for the design of therapies for neurodegenerative disorders such as Parkinson's disease.
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