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J Med Chem. 1989 Apr;32(4):841-6.

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

Author information

1
Orion Corporation Ltd., Orion Pharmaceutica, Research Laboratories, Espoo, Finland.

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.

PMID:
2704029
DOI:
10.1021/jm00124a017
[Indexed for MEDLINE]

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