Medizinische Universität Graz Austria/Österreich - Forschungsportal - Medical University of Graz
Gewählte Publikation:
SHR Neuro Krebs Kardio Lipid Stoffw Microb
Wube, AA; Hüfner, A; Thomaschitz, C; Blunder, M; Kollroser, M; Bauer, R; Bucar, F.
Design, synthesis and antimycobacterial activities of 1-methyl-2-alkenyl-4(1H)-quinolones.
Bioorg Med Chem. 2011; 19(1):567-579
Doi: 10.1016/j.bmc.2010.10.060
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- Co-Autor*innen der Med Uni Graz
- Kollroser Manfred
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- Abstract:
- A series of 23 new 1-methyl-2-alkenyl-4(1H)quinolones have been synthesized and evaluated in vitro for their antimycobacterial activities against fast growing species of mycobacteria, such as Mycobacterium fortuitum, M. smegmatis and M. phlei. The compounds displayed good to excellent inhibition of the growth of the mycobacterial test strains with improved antimycobacterial activity compared to the hit compound, evocarpine. The most active compounds, which possessed chain length of 11-13 carbons at position-2 displayed potent inhibitory effects with an MIC value of 1.0mg/L. In a human diploid embryonic lung cell line, MRC-5 cytotoxicity assay, the alkaloids showed weak to moderate cytotoxic activity. Biological evaluation of these evocarpine analogues on the less pathogenic fast growing strains of mycobacteria showed an interesting antimycobacterial profile and provided significant insight into the structure-activity relationships.
- Find related publications in this database (using NLM MeSH Indexing)
- Antitubercular Agents - chemical synthesis
- Cell Line -
- Drug Screening Assays, Antitumor -
- Humans -
- Magnetic Resonance Spectroscopy -
- Microbial Sensitivity Tests -
- Quinolones - chemical synthesis
- Find related publications in this database (Keywords)
- 1-Methyl-2-alkenyl-4(1H)-quinolone
- Antimycobacterial
- Tuberculosis
- SAR