4.5 Article

New L-dopa codrugs as potential antiparkinson agents

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ARCHIV DER PHARMAZIE
卷 341, 期 7, 页码 412-417

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WILEY-BLACKWELL
DOI: 10.1002/ardp.200700228

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caffeic acid; carnosine; L-dopa; L-dopa codrugs; Parkinson's disease

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This paper reports the synthesis and preliminary evaluation of new L-dopa (LD) conjugates (1 and 2) obtained by joining LD with two different natural antioxidants, caffeic acid and carnosine, respectively. The antioxidant efficacy of compounds 1 and 2 was assessed by evaluating plasmatic activities of superoxide dismutase (SOD) and glutathione peroxidase (GPx) in the rat. Rat striatal concentration of LD and dopamine (DA), and central nervous effects were evaluated after oral administration of the codrugs 1 and 2. The results suggest that, though our codrugs are devoid of significant antioxidant activity, they are able to induce sustained delivery of DA in rat striatum and can improve LD and DA release in the brain.

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