Design, synthesis and biological evaluation of l-dopa amide derivatives as potential prodrugs for the treatment of Parkinson’s disease

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.

Graphical abstractA range of amide derivatives of l-dopa were synthesized and investigated for their pharmacological activity and their ability to be converted to l-dopa in the unilaterally 6-hydroxydopamine (6-OHDA)-lesioned rat, as an experimental model of Parkinson’s disease.Figure optionsDownload full-size imageDownload as PowerPoint slide