4.7 Article

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

Journal

BIOORGANIC & MEDICINAL CHEMISTRY
Volume 22, Issue 1, Pages 381-392

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2013.11.012

Keywords

Dopamine receptor agonist; Parkinson's disease; Rotigotine

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The synthesis of a novel series of dopamine receptor agonists are described as well as their in vitro potency and efficacy on dopamine D-1 and D-2 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-1 and D-2 receptor profile similar to that of the most recently approved drug for Parkinson's disease, rotigotine. (C)2013 Elsevier Ltd. All rights reserved.

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