Synthesis and biological studies of glycosyl dopamine derivatives as potential antiparkinsonian agents.
A new approach to deliver dopamine into the central nervous system, based on the use of D-glucose as transportable agent, has been studied. Glycosyl dopamine derivatives bearing the sugar moiety linked to either the amino group or the catechol ring of dopamine through amide, ester or glycosidic bonds were synthesised as potential antiparkinsonian agents. Studies on the binding to dopamine D2 receptor, in vitro stability, and locomotive effect in mice of the synthetic glycoconjugates are reported.
Fernández
C
C
Instituto de Química Orgánica General, CSIC, Madrid, Spain.
Nieto
O
O
Rivas
E
E
Montenegro
G
G
Fontenla
J A
JA
Fernández-Mayoralas
A
A
D000818:Animals; D001667:Binding, Competitive; D001682:Biological Availability; D001692:Biological Transport; D001812:Blood-Brain Barrier; D004298:Dopamine / Q000031:analogs & derivatives / Q000138:chemical synthesis; D015259:Dopamine Agents / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D004355:Drug Stability; D005947:Glucose / Q000737:chemistry; D006027:Glycosides / Q000737:chemistry; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D010300:Parkinson Disease / Q000188:drug therapy*; D011355:Prodrugs / Q000138:chemical synthesis / Q000494:pharmacology; D051381:Rats; D017448:Receptors, Dopamine D2 / Q000378:metabolism
D015259:Dopamine Agents; D006027:Glycosides; D011355:Prodrugs; D017448:Receptors, Dopamine D2; D005947:Glucose; D004298:Dopamine