title: Design, synthesis and biological evaluation of peptide derivatives of L-dopa as anti-parkinsonian agents.
abstract: A series of dipeptide derivatives of L-dopa were synthesized and investigated for their pharmacological activity using the unilaterally 6-hydroxydopamine (6-OHDA)-lesioned rat as an experimental model of Parkinson's disease. Among them, (S)-isopropyl 2-(2-amino-2-methylpropanamido)-3-(3,4-dihydroxyphenyl)propanoate (4 g) was found to be the most active compound, with 106% AUC activity and 149% peak activity of L-dopa after oral administration.
authors: School of Food Science and Biotechnology, Zhejiang Gongshang University, Hangzhou, Zhejiang 310035, PR China. taozhou@zjgsu.edu.cn
authors: Tao
authors: T
authors: Zhou
authors: Robert C
authors: RC
authors: Hider
authors: Peter
authors: P
authors: Jenner
authors: Bruce
authors: B
authors: Campbell
authors: Christopher J
authors: CJ
authors: Hobbs
authors: Sarah
authors: S
authors: Rose
authors: Mark
authors: M
authors: Jairaj
authors: Kayhan A
authors: KA
authors: Tayarani-Binazir
authors: Alexander
authors: A
authors: Syme
mesh_terms: D000818:Animals; D000978:Antiparkinson Agents / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000494:pharmacology; D004151:Dipeptides / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000494:pharmacology; D004195:Disease Models, Animal; D015195:Drug Design; D007980:Levodopa / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology; D008297:Male; D015394:Molecular Structure; D009043:Motor Activity / Q000187:drug effects; D010455:Peptides / Q000008:administration & dosage / Q000138:chemical synthesis / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar
chemical_list: D000978:Antiparkinson Agents; D004151:Dipeptides; D010455:Peptides; C587538:isopropyl 2-(2-amino-2-methylpropanamido)-3-(3,4-dihydroxyphenyl)propanoate; D007980:Levodopa
keywords: 6-Hydroxydopamine (6-OHDA) lesioned rat; Parkinson’s disease; Prodrug; l-Dopa