39101-99-0Relevant articles and documents
Design and synthesis of a novel L-Dopa - Entacapone codrug
Lepp?nen, Jukka,Huuskonen, Juhani,Nevalainen, Tapio,Gynther, Jukka,Taipale, Hannu,J?rvinen, Tomi
, p. 1379 - 1382 (2002)
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 [t1/2 = 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 (t1/2 = 7 min; pH 7.4) at 37°C. The therapeutical potential of this novel codrug is discussed.