Department of Biology, New Mexico Institute of Mining and Technology, Socorro, NM 87801, USA.
Bioorg Med Chem Lett. 2011 Aug 15;21(16):4720-3. doi: 10.1016/j.bmcl.2011.06.081. Epub 2011 Jun 25.
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.
发现了吲哚与芳基重氮盐的新型反应,生成了 2-芳基-3-(芳偶氮基)吲哚。发现这些产物具有很强的抗耐甲氧西林金黄色葡萄球菌(MRSA)和抗利奈唑胺肠球菌(LLVRE)活性。SAR 研究表明,潜在的代谢不稳定的偶氮官能团可以被醚氧和硫醚硫原子取代,而不会损失任何活性。