| Autor: |
A E, Medvedev, R R, Ramsay, A S, Ivanov, A V, Veselovsky, V I, Shvedov, O V, Tikhonova, A P, Barradas, C K, Davidson, T A, Moskvitina, O A, Fedotova, L N, Axenova |
| Rok vydání: |
1999 |
| Předmět: |
|
| Zdroj: |
Neurobiology (Budapest, Hungary). 7(2) |
| ISSN: |
1216-8068 |
| Popis: |
A series of pirlindole analogues were tested as inhibitors of monoamine oxidase A and B. Although we did not find strict dependence between 3D-size of molecules and their inhibitory potency, rigid analogues exhibited potent and selective inhibition of MAO-A. They have 3D size limits of 13 angstroms (length) x 7 angstroms (height) x 4.4 angstroms (widths). Besides MAO-A inhibition flexible analogues also demonstrated potent inhibition of MAO-B. Five compounds were studied as inhibitors of purified human liver MAO-A. Their inhibitory potencies coincided with those obtained using rat liver mitochondrial MAO-A. Each compound induced changes in the spectrum of MAO-A but these did not correlate with the flexibility of the derivative. It is also possible that the oxygen bridge introduced with the flexibility might influence spectral patterns. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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