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

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R. Risgaard, M. Jensen, M. Jørgensen, B. Bang-Andersen, C.T. Christoffersen, Klaus Gervig Jensen, Jesper Langgaard Kristensen, A. Püschl

The synthesis of a novel series of dopamine receptor agonists are described as well as their in vitro potency and efficacy on dopamine D and D 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 D and D receptor profile similar to that of the most recently approved drug for Parkinson's disease, rotigotine.
Original languageEnglish
JournalBioorganic and Medicinal Chemistry
Issue number1
Pages (from-to)381-392
Publication statusPublished - 1 Jan 2014

ID: 93916376