title: Design and discovery of 1,3-benzodiazepines as novel dopamine antagonists.
abstract: A series of novel 1,3-benzodiazapine based D1 antagonists was designed according to the understanding of pharmacophore models derived from SCH 23390 (1b), a potent and selective D1 antagonist. The new design features an achiral cyclic-amidine that maintains desired basicity. Solid phase synthesis was developed for SAR development of the novel dopamine antagonists.
authors: Department of Medicinal Chemistry, Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. zhaoning.zhu@spcorp.com
authors: Zhaoning
authors: Z
authors: Zhu
authors: Zhong-Yue
authors: ZY
authors: Sun
authors: Yuanzan
authors: Y
authors: Ye
authors: Brian
authors: B
authors: McKittrick
authors: William
authors: W
authors: Greenlee
authors: Michael
authors: M
authors: Czarniecki
authors: Ahmad
authors: A
authors: Fawzi
authors: Hongtao
authors: H
authors: Zhang
authors: Jean E
authors: JE
authors: Lachowicz
mesh_terms: D001552:Benzazepines / Q000737:chemistry / Q000494:pharmacology; D001569:Benzodiazepines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D018492:Dopamine Antagonists / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D065127:Dopamine D2 Receptor Antagonists; D015195:Drug Design; D006801:Humans; D018377:Neurotransmitter Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D017447:Receptors, Dopamine D1 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D017448:Receptors, Dopamine D2 / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D001552:Benzazepines; D018492:Dopamine Antagonists; D065127:Dopamine D2 Receptor Antagonists; D018377:Neurotransmitter Agents; D017447:Receptors, Dopamine D1; D017448:Receptors, Dopamine D2; C534628:SCH 23390; D001569:Benzodiazepines