Remote functionalization of SCH 39166: Discovery of potent and selective benzazepine dopamine D₁ receptor antagonists

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• 作者：T.K. Sasikumar ; Duane A. Burnett ; William J. Greenlee ; Michelle Smith ; Ahmad Fawzi ; Hongtao Zhang ; Jean E. Lachowicz
• 关键词：SCH 39166 ; Ecopipam ; Benzazepine ; Dopamine antagonist ; Obesity
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2010
• 出版时间：1 February 2010
• 年：2010
• 卷：20
• 期：3
• 页码：832-835
• 全文大小：506 K

文摘

A series of novel benzazepine derived dopamine D₁ antagonists have been discovered. These compounds are highly potent at D₁ and showed excellent selectivity over D₂ and D₄ receptors. SAR studies revealed that a variety of functional groups are tolerated on the D-ring of known tetracyclic benzazepine analog 2, SCH 39166, leading to compounds with nanomolar potency at D₁ and good selectivity over D₂-like receptors.