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Bisubstrate Inhibitors of the Enzyme Catechol O-Methyltransferase (COMT): Efficient Inhibition Despite the Lack of a Nitro Group

✍ Scribed by Ralph Paulini; Christian Lerner; Roland Jakob-Roetne; Gerhard Zürcher; Edilio Borroni; François Diederich

Publisher
John Wiley and Sons
Year
2004
Tongue
English
Weight
188 KB
Volume
5
Category
Article
ISSN
1439-4227

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## Abstract Inhibition of the enzyme catechol __O__‐methyltransferase (COMT) is of significant interest in the therapy of __Parkinson__'s disease. Described herein are structural analogs of the potent bisubstrate inhibitor (−)‐1 (__IC__~50~=9 nM; __Table 1__) for COMT, with target modifications of