Potential metabolites of a condensed 2,3-benzodiazepine derivative

详细信息    查看全文

• 作者：Emese Csuzdi ; Katalin Miglé ; czi ; Istvá ; n Hazai ; Pá ; l Berzsenyi ; Istvá ; n Pallagi ; Gyula Horvá ; th ; Gyö ; rgy Lengyel and Sá ; ndor Só ; lyom
• 关键词：AMPA antagonist ; Imidazole[ ; 2 ; 3] ; benzodiazepine ; Metabolite ; HPLC/MS analysis
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2005
• 出版时间：2005
• 年：2005
• 卷：15
• 期：21
• 页码：4662-4665
• 全文大小：114 K

文摘

Putative metabolites of an AMPA antagonist imidazo-2,3-benzodiazepine (2) were synthesized and compared to constituents formed from the parent compound by a rat liver perfusion method. As metabolic transformations, hydroxylation of the 2-methyl group and N-acetylation of the amino functionality in parent compound (2) were registered. The hydroxylated analogue 12 of 2 exhibits a weak AMPA antagonist activity.