Hit-to-lead optimization of pyrrolo[1,2-a

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• 作者：Gyö ; rgy Szabó ; Ró ; bert Kiss ; Dó ; ra Pá ; yer-Lengyel ; Krisztina Vukics ; Judit Szikra ; Andrea Baki ; Lá ; szló ; Molná ; r ; Já ; nos Fischer ; Gyö ; rgy M. Keserű
• 关键词：CB1 receptor ; Rimonabant ; Hit-to-lead ; SAR ; Pyrrolo[1 ; 2-a]quinoxaline
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2009
• 出版时间：1 July 2009
• 年：2009
• 卷：19
• 期：13
• 页码：3471-3475
• 全文大小：373 K

文摘

Hit-to-lead optimization of a novel series of N-alkyl-N-[2-oxo-2-(4-aryl-4H-pyrrolo[1,2-a]quinoxaline-5-yl)-ethyl]-carboxylic acid amides, derived from a high throughput screening (HTS) hit, are described. Subsequent optimization led to identification of in vitro potent cannabinoid 1 receptor (CB1R) antagonists representing a new class of compounds in this area.