2. Academic Validation
  3. Anti-tuberculosis activity and structure-activity relationships of oxygenated tricyclic carbazole alkaloids and synthetic derivatives

Anti-tuberculosis activity and structure-activity relationships of oxygenated tricyclic carbazole alkaloids and synthetic derivatives

  • Bioorg Med Chem. 2017 Nov 15;25(22):6167-6174. doi: 10.1016/j.bmc.2016.12.038.
Carsten Börger 1,  Christian Brütting 1,  Konstanze K Julich-Gruner 1,  Ronny Hesse 1,  V Pavan Kumar 1,  Sebastian K Kutz 1,  Marika Rönnefahrt 1,  Claudia Thomas 1,  Baojie Wan 2,  Scott G Franzblau 2,  Hans-Joachim Knölker 3
Affiliations

Affiliations

  • 1 Department Chemie, Technische Universität Dresden, Bergstraße 66, 01069 Dresden, Germany.
  • 2 Institute for Tuberculosis Research, College of Pharmacy, University of Illinois at Chicago, 833 S. Wood St., MC 964, Chicago, IL 60612-7231, USA.
  • 3 Department Chemie, Technische Universität Dresden, Bergstraße 66, 01069 Dresden, Germany. Electronic address: hans-joachim.knoelker@tu.dresden.de.
PMID: 28094223 DOI: 10.1016/j.bmc.2016.12.038
Abstract

A series of 49 oxygenated tricyclic carbazole derivatives has been tested for inhibition of the growth of Mycobacterium tuberculosis and a mammalian cell line (vero cells). From this series, twelve carbazoles showed a significant anti-TB activity. The four most active compounds were the naturally occurring Carbazole Alkaloids clauszoline-M (45), murrayaline-C (41), carbalexin-C (27), and the synthetic carbazole derivative 22 with MIC90 values ranging from 1.5 to 3.7μM. The active compounds were virtually nontoxic for the mammalian cell line in the concentration range up to 50μM.

Keywords

Alkaloids; Anti-TB activity; Carbazoles; Natural products; Tuberculosis.

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