Synthesis and Anti-Tuberculosis Activity of Olivacine and Oxygenated Derivatives

Ulrike Schmidt; Gabriele Theumer; Anne Jäger; Olga Kataeva; Baojie Wan; Scott G. Franzblau; Hans-Joachim Knölker

doi:10.20944/preprints201805.0040.v1

Version 1 : Received: 30 April 2018 / Approved: 2 May 2018 / Online: 2 May 2018 (12:54:38 CEST)
Version 2 : Received: 31 May 2018 / Approved: 1 June 2018 / Online: 1 June 2018 (09:39:56 CEST)

A peer-reviewed article of this Preprint also exists.

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. 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.

Journal reference: Molecules 2018, 23, 1402
DOI: 10.3390/molecules23061402

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 key step. In a test for inhibition of the growth of Mycobacterium tuberculosis 9-methoxyolivacine showed the most significant anti-TB activity with an MIC₉₀ value of 1.5 μM.

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Synthesis and Anti-Tuberculosis Activity of Olivacine and Oxygenated Derivatives

Abstract

Keywords

Subject

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