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Investigation of Pyrazolo[1,5-a]quinoxalin-4-ones as Novel Monoamine Oxidase Inhibitors by Panova, Valeria A.; Filimonov, Sergey I.; Chirkova, Zhanna V.; Kabanova, Mariya V.; Shetnev, Anton A.; Korsakov, Mikhail K.; Petzer, Anél; Petzer, Jacobus P.; Suponitsky, Kyrill Yu is a Chemistry article available to read on EtoBox.
What is Investigation of Pyrazolo[1,5-a]quinoxalin-4-ones as Novel Monoamine Oxidase Inhibitors about?
The monoamine oxidase (MAO) enzymes are key metabolic enzymes of neurotransmitter and other bioactive amines, and represent important drug targets for the treatment of neuropsychiatric and neurodegenerative disorders. Inhibitors of MAO are established medications for the treatment of depression and Parkinson's disease, and may have future roles in other disease states such as the therapy of prostate cancer, cardiovascular disease and inflammatory diseases. Based on these considerations, the present study synthesizes a series of 22 pyrazolo[1,5-a]quinoxalin-4-one derivatives and evaluated them as potential inhibitors of human MAO-A and MAO-B. The results show that 8 derivatives inhibit MAO-A, and 3 derivatives inhibit MAO-B with IC values in the submicromolar range (<1 μM). The most potent MAO-A inhibitor, N-[5-(acetyloxy)-2-(4-chlorophenyl)-4-oxo-4,5-dihydropyrazolo[1,5-a]quinoxalin-7-yl]acetamide (7c), exhibit an IC value of 0.028 μM and displays 50-fold selectivity for MAO-A over MAO-B. The most potent MAO-B inhibitor, 2-(4-methylphenyl)-4-oxo-4,5-dihydropyrazolo[1,5-a]quinoxaline-7-carbonitrile (4f), exhibit an IC value of 0.617 μM and displays 8-fold selectivity for MAO-B. This
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- Author
- Panova, Valeria A.; Filimonov, Sergey I.; Chirkova, Zhanna V.; Kabanova, Mariya V.; Shetnev, Anton A.; Korsakov, Mikhail K.; Petzer, Anél; Petzer, Jacobus P.; Suponitsky, Kyrill Yu
- Publisher
- Elsevier Science; Elsevier ; Elsevier Inc.; Elsevier BV (ISSN 0045-2068)
- Published
- 2020
- Language
- EN
- Field
- Chemistry (Physical Sciences)