title: Design, synthesis and biological evaluation of L-dopa amide derivatives as potential prodrugs for the treatment of Parkinson's disease.
abstract: A range of amide derivatives of L-dopa were synthesized and investigated for their pharmacological activity and their ability to be converted to L-dopa using the unilaterally 6-hydroxydopamine (6-OHDA)-lesioned rat, as an experimental model of Parkinson's disease. The diacetyl derivative of L-dopa amide (11b) was found to be more active than L-dopa after its oral administration and generated plasma levels of L-dopa in the therapeutic range for an antiparkinsonian effect in man.
authors.affiliation: School of Food Science and Biotechnology, Zhejiang Gongshang University, Hangzhou, Zhejiang, 310035, PR China.
authors.forename: Tao
authors.initials: T
authors.lastname: Zhou
authors.forename: Robert C
authors.initials: RC
authors.lastname: Hider
authors.forename: Peter
authors.initials: P
authors.lastname: Jenner
authors.forename: Bruce
authors.initials: B
authors.lastname: Campbell
authors.forename: Christopher J
authors.initials: CJ
authors.lastname: Hobbs
authors.forename: Sarah
authors.initials: S
authors.lastname: Rose
authors.forename: Mark
authors.initials: M
authors.lastname: Jairaj
authors.forename: Kayhan A
authors.initials: KA
authors.lastname: Tayarani-Binazir
authors.forename: Alexander
authors.initials: A
authors.lastname: Syme
mesh_terms: D000577:Amides / Q000737:chemistry*; D000818:Animals; D015195:Drug Design; D007980:Levodopa / Q000737:chemistry* / Q000378:metabolism / Q000493:pharmacokinetics / Q000494:pharmacology*; D008297:Male; D016627:Oxidopamine / Q000494:pharmacology; D010300:Parkinson Disease / Q000188:drug therapy* / Q000209:etiology; D011355:Prodrugs / Q000737:chemistry* / Q000378:metabolism / Q000493:pharmacokinetics / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar
chemical_list: D000577:Amides; D011355:Prodrugs; D007980:Levodopa; D016627:Oxidopamine