Unprecedented C-2 arylation of indole with diazonium salts: Syntheses of 2,3-disubstituted indoles and their antimicrobial activity

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• 作者：Seth Daly^a ; Kathryn Hayden^a ; Indranil Malik^a ; Nikki Porch^a ; Hong Tang^a ; Snezna Rogelj^a ; Liliya V. Frolova^b ; Katrina Lepthien^b ; Alexander Kornienko^b ; Igor V. Magedov^b ; ^{imagedov@nmt.edu"" rel=""nofollow}
• 关键词：MRSA ; Low-level VRE ; Indole ; Arylation
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2011
• 出版时间：15 August 2011
• 年：2011
• 卷：21
• 期：16
• 页码：4720-4723
• 全文大小：398 K

文摘

A novel reaction of indole with aryldiazonium salts leading to the formation of 2-aryl-3-(arylazo)indoles was discovered. The products were found to possess potent anti-MRSA and anti-LLVRE activities. The SAR studies indicate that the potentially metabolically labile azo functionality can be replaced with ether oxygen and thioether sulfur atoms without any loss of activity.