Document Report Card

ID: ALA1124446

Journal: J Med Chem

Title: Synthesis of some novel potent and selective catechol O-methyltransferase inhibitors.

Authors: Bäckström R, Honkanen E, Pippuri A, Kairisalo P, Pystynen J, Heinola K, Nissinen E, Linden IB, Männistö PT, Kaakkola S.

Abstract: 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.

CiteXplore: 2704029

DOI: 10.1021/jm00124a017