Bioorganic and Medicinal Chemistry Letters p. 2859 - 2864 (1998)
Update date:2022-08-03
Topics:
Avenell, Kim Y.
Boyfield, Izzy
Coldwell, Martyn C.
Hadley, Michael S.
Healy, Maureen A. M.
Jeffrey, Philip M.
Johnson, Christopher N.
Nash, David J.
Riley, Graham J.
Scott, Emma E.
Smith, Stephen A.
Stacey, Rachel
Stemp, Geoffrey
Thewlis, Kevin M.
Starting from a series of 2-aminotetralins 1, a novel series of N-[4- (4-phenylbenzoylamino)butyl]-octahydrobenzoquinolines and hexahydrobenzoindoles with high potency and selectivity for the dopamine D3 receptor has been designed. The effect of ligand chirality on binding affinity has been established. Selected derivatives (e.g. 2o, 2p) show high functional selectivity and enhanced in vivo properties compared to 1.
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