Dimeric l-Dopa Derivatives as Potential Prodrugs

A series of dimeric derivatives (+)- 1, and (+)- 2, and (+)- 3a–d of l-Dopa diacetyl esters was synthesized and evaluated as potential l-Dopa prodrugs with improved physicochemical properties. All the new compounds showed chemical stability in aqueous buffer solutions (pH 1.3 and 7.4). A relatively...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2001-04, Vol.11 (8), p.1085-1088
Hauptverfasser:	Di Stefano, Antonio, Mosciatti, Barbara, Mario Cingolani, Gian, Giorgioni, Gianfabio, Ricciutelli, Massimo, Cacciatore, Ivana, Sozio, Piera, Claudi, Francesco
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Anticonvulsants. Antiepileptics. Antiparkinson agents Biological and medical sciences Dimerization Drug Stability Half-Life Humans Hydrogen-Ion Concentration Hydrolysis Levodopa - analogs & derivatives Levodopa - chemical synthesis Levodopa - pharmacokinetics Medical sciences Neuropharmacology Pharmacology. Drug treatments Plasma - metabolism Prodrugs - chemical synthesis Prodrugs - pharmacokinetics Rats
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Zusammenfassung:	A series of dimeric derivatives (+)- 1, and (+)- 2, and (+)- 3a–d of l-Dopa diacetyl esters was synthesized and evaluated as potential l-Dopa prodrugs with improved physicochemical properties. All the new compounds showed chemical stability in aqueous buffer solutions (pH 1.3 and 7.4). A relatively slow release of l-Dopa in human plasma was observed. A series of dimeric derivatives (+)-1, (+)-2, and (+)-3a–d of l-Dopa diacetyl esters was synthesized and evaluated as potential prodrugs with improved physicochemical properties. A relatively slow release of l-Dopa in human plasma was observed.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(01)00140-8