TY - JOUR
T1 - Synthesis and SAR study of a novel series of dopamine receptor agonists
AU - Risgaard, R.
AU - Jensen, M.
AU - Jørgensen, M.
AU - Bang-Andersen, B.
AU - Christoffersen, C.T.
AU - Jensen, Klaus Gervig
AU - Kristensen, Jesper Langgaard
AU - Püschl, A.
PY - 2014/1/1
Y1 - 2014/1/1
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=84888329541&partnerID=8YFLogxK
U2 - 10.1016/j.bmc.2013.11.012
DO - 10.1016/j.bmc.2013.11.012
M3 - Journal article
C2 - 24296012
SN - 0968-0896
VL - 22
SP - 381
EP - 392
JO - Bioorganic and Medicinal Chemistry
JF - Bioorganic and Medicinal Chemistry
IS - 1
ER -