Design, synthesis and biological evaluation of l-dopa amide derivatives as potential prodrugs for the treatment of Parkinson’s disease
| Autor: | Sarah Rose, Robert C. Hider, Bruce Campbell, Kayhan A. Tayarani-Binazir, Christopher Hobbs, Alexander Syme, Mark Jairaj, Tao Zhou, Peter Jenner |
|---|---|
| Rok vydání: | 2010 |
| Předmět: |
Male
Levodopa Parkinson's disease Stereochemistry Chemical synthesis chemistry.chemical_compound Therapeutic index Oral administration Amide Drug Discovery medicine Animals Prodrugs Rats Wistar Oxidopamine Pharmacology Organic Chemistry Parkinson Disease Biological activity General Medicine Prodrug medicine.disease Amides Rats nervous system diseases chemistry Drug Design medicine.drug |
| Zdroj: | European Journal of Medicinal Chemistry. 45:4035-4042 |
| ISSN: | 0223-5234 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect