Synthesis of some novel potent and selective catechol O-methyltransferase inhibitors
| Autor: | R, Bäckström, E, Honkanen, A, Pippuri, P, Kairisalo, J, Pystynen, K, Heinola, E, Nissinen, I B, Linden, P T, Männistö, S, Kaakkola |
|---|---|
| Rok vydání: | 1989 |
| Předmět: |
Chemical Phenomena
Stereochemistry Catechols COMT inhibitor behavioral disciplines and activities Binding Competitive chemistry.chemical_compound Structure-Activity Relationship mental disorders Drug Discovery Animals IC50 chemistry.chemical_classification Catechol fungi Brain Catechol O-Methyltransferase Inhibitors Rats Inbred Strains Metabolism In vitro Nitecapone Rats Chemistry Enzyme nervous system chemistry Catechol-O-Methyltransferase Inhibitors Molecular Medicine Female |
| Zdroj: | Journal of medicinal chemistry. 32(4) |
| ISSN: | 0022-2623 |
| Popis: | A series of disubstituted catechol derivatives was synthesized and tested as potential COMT inhibitors. The most active compounds were more than 1000 times more potent (IC50 = 3-6 nM) in vitro than the known COMT inhibitor, 3',4'-dihydroxy-2-methylpropiophenone (U 0521, IC50 = 6000 nM). The new compounds were also highly selective COMT inhibitors with no activity against other essential enzymes involved in the synthesis and metabolism of catecholamines. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|