Unprecedented C-2 arylation of indole with diazonium salts: Syntheses of 2,3-disubstituted indoles and their antimicrobial activity
作者:Seth Daly、Kathryn Hayden、Indranil Malik、Nikki Porch、Hong Tang、Snezna Rogelj、Liliya V. Frolova、Katrina Lepthien、Alexander Kornienko、Igor V. Magedov
DOI:10.1016/j.bmcl.2011.06.081
日期:2011.8
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. (C) 2011 Elsevier Ltd. All rights reserved.