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

European Journal of Medicinal Chemistry
Tao ZhouAlexander Syme

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.

Citations

Mar 16, 2011·European Journal of Drug Metabolism and Pharmacokinetics·Nuggehally R Srinivas
Apr 13, 2012·Expert Opinion on Drug Discovery·Piera SozioAntonio Di Stefano
Dec 1, 2017·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Monique HoonAnél Petzer
Jan 4, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Fatma HaddadRafik Karaman
Jun 20, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Chunying MaWenhua Feng
Jan 25, 2018·Expert Opinion on Drug Discovery·Ivana CacciatoreAntonio Di Stefano
Aug 27, 2013·Bioorganic & Medicinal Chemistry Letters·Tao ZhouAlexander Syme

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