Molecules
(Jun 2018)
Synthesis and Activity against Mycobacterium tuberculosis of Olivacine and Oxygenated Derivatives
Ulrike Schmidt,
Gabriele Theumer,
Anne Jäger,
Olga Kataeva,
Baojie Wan,
Scott G. Franzblau,
Hans-Joachim Knölker
Affiliations
Ulrike Schmidt
Faculty of Chemistry, Technische Universität Dresden, Bergstraße 66, 01069 Dresden, Germany
Gabriele Theumer
Faculty of Chemistry, Technische Universität Dresden, Bergstraße 66, 01069 Dresden, Germany
Anne Jäger
Faculty of Chemistry, Technische Universität Dresden, Bergstraße 66, 01069 Dresden, Germany
Olga Kataeva
A. M. Butlerov Chemistry Institute, Kazan Federal University, Kremlevskaya Str. 18, Kazan 420008, Russia
Baojie Wan
Institute for Tuberculosis Research, College of Pharmacy, University of Illinois at Chicago, 833 S. Wood St., MC 964, Chicago, IL 60612-7231, USA
Scott G. Franzblau
Institute for Tuberculosis Research, College of Pharmacy, University of Illinois at Chicago, 833 S. Wood St., MC 964, Chicago, IL 60612-7231, USA
Hans-Joachim Knölker
Faculty of Chemistry, Technische Universität Dresden, Bergstraße 66, 01069 Dresden, Germany
DOI
https://doi.org/10.3390/molecules23061402
Journal volume & issue
Vol. 23,
no. 6
Abstract
Read online
The tetracyclic pyrido[4,3-b]carbazole olivacine and four of its oxygenated derivatives have been synthesized by a late-stage palladium-catalyzed Heck-type cyclization of the pyrrole ring as a key step. In a test for the inhibition of the growth of Mycobacterium tuberculosis, 9-methoxyolivacine showed the most significant inhibitory activity against Mycobacterium tuberculosis, with an MIC90 value of 1.5 μM.
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