Anti-tuberculosis activity and structure–activity relationships of oxygenated tricyclic carbazole alkaloids and synthetic derivatives
| Autor: | Ronny Hesse, Christian Brütting, Scott G. Franzblau, Claudia Thomas, Sebastian K. Kutz, Marika Rönnefahrt, Hans-Joachim Knölker, Carsten Börger, V. Pavan Kumar, Konstanze K. Julich-Gruner, Baojie Wan |
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| Rok vydání: | 2017 |
| Předmět: |
Synthetic derivatives
Cell Survival Stereochemistry Clinical Biochemistry Antitubercular Agents Carbazoles Pharmaceutical Science Microbial Sensitivity Tests 010402 general chemistry 01 natural sciences Biochemistry Mycobacterium tuberculosis Structure-Activity Relationship chemistry.chemical_compound Alkaloids Anti tuberculosis Mammalian cell Chlorocebus aethiops Drug Discovery Animals Organic chemistry Structure–activity relationship Vero Cells Molecular Biology chemistry.chemical_classification biology 010405 organic chemistry Carbazole Organic Chemistry biology.organism_classification 0104 chemical sciences chemistry Vero cell Molecular Medicine Tricyclic |
| Zdroj: | Bioorganic & Medicinal Chemistry. 25:6167-6174 |
| ISSN: | 0968-0896 |
| DOI: | 10.1016/j.bmc.2016.12.038 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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