Synthesis of some novel potent and selective catechol O-methyltansferase inhibitors

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 (IC sub(50) = 3-6 nM) in vitro than the known COMT inhibitor, 3',4'-dihydroxy-2-methylpropiophenone (U 0521, IC sub(50) =...

Full description

Saved in:
Bibliographic Details
Published inJournal of medicinal chemistry Vol. 32; no. 4; pp. 841 - 846
Main Authors Baeckstroem, R, Honkanen, E, Pippuri, A, Kairisalo, P, Pystynen, J, Heinola, K, Nissinen, E, Linden, L B, Maennistoe, P T
Format Journal Article
LanguageEnglish
Published 01.01.1989
Subjects
catechol
Online AccessGet full text

Cover

More Information
Summary: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 (IC sub(50) = 3-6 nM) in vitro than the known COMT inhibitor, 3',4'-dihydroxy-2-methylpropiophenone (U 0521, IC sub(50) = 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.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
content type line 23
ObjectType-Feature-2
ISSN:0022-2623