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Natural product leads for drug discovery: Isolation,synthesis and biological evaluation of 6-cyano-5-methoxyindolo[2,3-a]carbazole based ligands as antibacterial agents
Authors:Songpo Guo  Suresh K Tipparaju  Scott D Pegan  Baojie Wan  Shunyan Mo  Jimmy Orjala  Andrew D Mesecar  Scott G Franzblau  Alan P Kozikowski
Institution:1. Drug Discovery Program, Department of Medicinal Chemistry and Pharmacognosy, University of Illinois at Chicago, 833 S. Wood Street, Chicago, USA;2. Center for Pharmaceutical Biotechnology, University of Illinois at Chicago, 900 S. Ashland Avenue, Chicago, USA;3. Institute for Tuberculosis, Research College of Pharmacy, University of Illinois at Chicago, 833 S. Wood Street, Chicago, USA
Abstract:Indolo2,3-a]carbazole based inhibitors were synthesized from readily available indigo via a seven-step linear synthetic sequence with a moderate overall yield. The inhibitors were selectively and readily functionalized at the nitrogen on the indole portion of the carbazole unit. The synthesized analogs displayed moderate inhibitory activities toward Bacillus anthracis and Mycobacterium tuberculosis, indicating that indolo2,3-a]carbazoles could serve as promising leads in the development of new drugs to combat anthrax and tuberculosis infections.
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