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

…, E Honkanen, A Pippuri, P Kairisalo…

文献索引：Baeckstroem, Reijo; Honkanen, Erkki; Pippuri, Aino; Kairisalo, Pekka; Pystynen, Jarmo; et al. Journal of Medicinal Chemistry, 1989 , vol. 32, # 4 p. 841 - 846

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被引用次数: 158

摘要

A series of disubstituted catechol derivatives was synthesized and tested as potential COMT inhibitors. The most active compounds were more than loo0 times more potent (ICm= 3-6 nM) in vitro than the known COMT inhibitor, 3', 4'-dihydroxy-2-methylpropiophenone (U 0521, ICm= 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 ...