Catechol O-methyltransferase. 8. Structure-activity relationships for inhibtion by 8-hydroxyquinolines.
A series of 5- and 7-substituted 8-hydroxyquinolines was evaluated as inhibitors of catechol O-methyltransferase (COMT, E.C. 2.1.1.6). The electronic character of the substituents in the 5 position appeared to have only a small effect if any on the inhibitory activity of these compounds. A significant factor which contributes to the inhibitory activity of these compounds appears to be the nature of the 7-substituent. The structure-activity relationship for this series of inhibitors is discussed relative to the nature of the enzymatic binding site.
D000818:Animals; D065098:Catechol O-Methyltransferase Inhibitors; D006912:Hydroxyquinolines / Q000138:chemical synthesis*; D066298:In Vitro Techniques; D008099:Liver / Q000201:enzymology; D008297:Male; D015125:Oxyquinoline / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D012044:Regression Analysis; D013329:Structure-Activity Relationship
D065098:Catechol O-Methyltransferase Inhibitors; D006912:Hydroxyquinolines; D015125:Oxyquinoline