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Synthesis and Activity against Mycobacterium tuberculosis of Olivacine and Oxygenated Derivatives.

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 ?M.

SUBMITTER: Schmidt U

PROVIDER: S-EPMC6100493 | biostudies-literature | 2018 Jun

REPOSITORIES: biostudies-literature

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Synthesis and Activity against Mycobacterium tuberculosis of Olivacine and Oxygenated Derivatives.

Schmidt Ulrike U Theumer Gabriele G Jäger Anne A Kataeva Olga O Wan Baojie B Franzblau Scott G SG Knölker Hans-Joachim HJ

Molecules (Basel, Switzerland) 20180609 6

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. ...[more]

PMID: 29890747

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