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 μM.

Keywords

• inhibitory activity
• catalysis
• cyclization
• olivacine
• palladium
• pyrido[4,3-b]carbazoles