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ID: ALA1149426

Journal: Bioorg Med Chem Lett

Title: Synthesis and SAR of highly potent and selective dopamine D(3)-receptor antagonists: Quinolin(di)one and benzazepin(di)one derivatives. herve.geneste@abbott.com.

Authors: Geneste H, Backfisch G, Braje W, Delzer J, Haupt A, Hutchins CW, King LL, Lubisch W, Steiner G, Teschendorf HJ, Unger L, Wernet W.

Abstract: The synthesis and SAR of novel and selective dopamine D(3)-receptor antagonists based on a 3,4-dihydro-1H-quinolin-2-one, a 1,3,4,5-tetrahydro-benzo[b]azepin-2-one, 1H-quinoline-2,4-dione or a 3,4-dihydro-1H-benzo[b]azepine-2,5-dione scaffold are discussed. A706149 (2.15mg/kg, po) antagonizes PD 128907-induced huddling deficits in rat, a social interaction paradigm.

CiteXplore: 16271293

DOI: 10.1016/j.bmcl.2005.10.035