| Autor: |
Medvedev AE; Institute of Biomedical Chemistry, Russian Academy of Medical Sciences., Ivanov AS, Kamyshanskaya NS, Kirkel AZ, Moskvitina TA, Gorkin VZ, Li NY, Marshakov VYu |
| Jazyk: |
angličtina |
| Zdroj: |
Biochemistry and molecular biology international [Biochem Mol Biol Int] 1995 May; Vol. 36 (1), pp. 113-22. |
| Abstrakt: |
Indole and isatin (2,3-dioxindole) analogues were studied as inhibitors of MAO-A and B. They exhibited reversible and competitive MAO inhibition. Three dimensional structures of the compounds tested were constructed and minimized using PC-based molecular graphic software. The QSAR analysis revealed the requirement of co-planar structure of substituents at C2 and C3 of indole ring for selective MAO-A inhibition, whilst type of bond was less essential. The presence of hydroxy group at C5 of isatin increased selectivity of MAO-A inhibition, however simultaneous insertion of substituents into both positions of indole ring (5-hydroxy-2-phenylindole) led to a decrease of MAO-A inhibition. The planar molecules demonstrating potent MAO-A inhibition have the average sizes 7 A in length and 6 A in width. The MAO B inhibition also depended on the sizes of planar molecules however distribution of electron density in the molecules was another precondition for the selective inhibition of the enzyme. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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