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  • Title: Unprecedented C-2 arylation of indole with diazonium salts: Syntheses of 2,3-disubstituted indoles and their antimicrobial activity.
    Author: Daly S, Hayden K, Malik I, Porch N, Tang H, Rogelj S, Frolova LV, Lepthien K, Kornienko A, Magedov IV.
    Journal: Bioorg Med Chem Lett; 2011 Aug 15; 21(16):4720-3. PubMed ID: 21752646.
    Abstract:
    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.
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