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Molecules 2018, 23(6), 1402; https://doi.org/10.3390/molecules23061402

Synthesis and Activity against Mycobacterium tuberculosis of Olivacine and Oxygenated Derivatives

1
Faculty of Chemistry, Technische Universität Dresden, Bergstraße 66, 01069 Dresden, Germany
2
A. M. Butlerov Chemistry Institute, Kazan Federal University, Kremlevskaya Str. 18, Kazan 420008, Russia
3
Institute for Tuberculosis Research, College of Pharmacy, University of Illinois at Chicago, 833 S. Wood St., MC 964, Chicago, IL 60612-7231, USA
*
Author to whom correspondence should be addressed.
Received: 30 April 2018 / Revised: 31 May 2018 / Accepted: 6 June 2018 / Published: 9 June 2018
(This article belongs to the Section Organic Chemistry)
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Abstract

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. View Full-Text
Keywords: inhibitory activity; catalysis; cyclization; olivacine; palladium; pyrido[4,3-b]carbazoles inhibitory activity; catalysis; cyclization; olivacine; palladium; pyrido[4,3-b]carbazoles
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Schmidt, U.; Theumer, G.; Jäger, A.; Kataeva, O.; Wan, B.; Franzblau, S.G.; Knölker, H.-J. Synthesis and Activity against Mycobacterium tuberculosis of Olivacine and Oxygenated Derivatives. Molecules 2018, 23, 1402.

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