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Design and synthesis of a novel L-dopa-entacapone codrug
Jukka Leppänen1, Juhani Huuskonen, Tapio Nevalainen
1Department of Pharmaceutical Chemistry, University of Kuopio, P.O. Box 1627, 70211, Kuopio, Finland, and Finncovery Ltd., Kuopio, Finland. jukka.leppanan@uku.fi
Journal of Medicinal Chemistry
|March 8, 2002
Abstract:
A novel codrug, in which L-Dopa and entacapone are linked via a biodegradable carbamate spacer to form a single chemical entity, was synthesized and studied kinetically. This carbamate codrug provides adequate stability [t(1/2) = 12.1 h (pH 1.2); 1.4 h (pH 5.0); 1.1 h (pH 7.4)] against chemical hydrolysis but rapidly hydrolyzes to L-Dopa and entacapone in liver homogenate (t(1/2) = 7 min; pH 7.4) at 37 degrees C. The therapeutical potential of this novel codrug is discussed.