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. 2014 Jan 1;22(1):381-92.
doi: 10.1016/j.bmc.2013.11.012. Epub 2013 Nov 15.

Synthesis and SAR study of a novel series of dopamine receptor agonists

Rune Risgaard  1 , Martin Jensen  2 , Morten Jørgensen  2 , Benny Bang-Andersen  2 , Claus T Christoffersen  3 , Klaus G Jensen  3 , Jesper L Kristensen  4 , Ask Püschl  5
Affiliations

Synthesis and SAR study of a novel series of dopamine receptor agonists

Rune Risgaard et al. Bioorg Med Chem. .

Abstract

The synthesis of a novel series of dopamine receptor agonists are described as well as their in vitro potency and efficacy on dopamine D₁ and D₂ receptors. This series was designed from pergolide and (4aR,10aR)-1-propyl-1,2,3,4,4a,5,10,10a-octahydro-benzo[g]quinolin-6-ol (PHBQ) and resulted in the synthesis of (2R,4aR,10aR)-2-methylsulfanylmethyl-4-propyl-3,4,4a,5,10,10a-hexahydro-2H-naphtho[2,3-b][1,4]oxazin-9-ol (compound 27), which has a D₁ and D₂ receptor profile similar to that of the most recently approved drug for Parkinson's disease, rotigotine.

Keywords: Dopamine receptor agonist; Parkinson’s disease; Rotigotine.

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