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

Submitted:

30 April 2018

Posted:

02 May 2018

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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^*

A peer-reviewed article of this preprint also exists.

Submitted:

30 April 2018

Posted:

02 May 2018

Read the latest preprint version here

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.

Keywords:

anti-TB activity

;

catalysis

;

cyclization

;

olivacine

;

palladium

;

pyrido[4

;

3-b]carbazoles

Subject:

Chemistry and Materials Science - Organic Chemistry

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