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J Med Chem. 2002 Mar 14;45(6):1379-82.

Design and synthesis of a novel L-dopa-entacapone codrug.

Author information

1
Department of Pharmaceutical Chemistry, University of Kuopio, P.O. Box 1627, 70211, Kuopio, Finland, and Finncovery Ltd., Kuopio, Finland. jukka.leppanan@uku.fi

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.

PMID:
11882007
DOI:
10.1021/jm010980d
[Indexed for MEDLINE]

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