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New Non-Toxic Semi-Synthetic Derivatives from Natural Diterpenes Displaying Anti-Tuberculosis Activity

We report herein the synthesis of six diterpene derivatives, three of which are new, generated through known organic chemistry reactions that allowed structural modification of the existing natural products kaurenoic acid (1) and copalic acid (2). The new compounds were fully characterized using hig...

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Detalles Bibliográficos
Autores principales: Matos, Priscilla M., Mahoney, Brian, Chan, Yohan, Day, David P., Cabral, Mirela M. W., Martins, Carlos H. G., Santos, Raquel A., Bastos, Jairo K., Bulman Page, Philip C., Heleno, Vladimir C. G.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2015
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6331924/
https://www.ncbi.nlm.nih.gov/pubmed/26457701
http://dx.doi.org/10.3390/molecules201018264
Descripción
Sumario:We report herein the synthesis of six diterpene derivatives, three of which are new, generated through known organic chemistry reactions that allowed structural modification of the existing natural products kaurenoic acid (1) and copalic acid (2). The new compounds were fully characterized using high resolution mass spectrometry, infrared spectroscopy, (1)H- and (13)C-NMR experiments. We also report the evaluation of the anti-tuberculosis potential for all compounds, which showed some promising results for Micobacterium tuberculosis inhibition. Moreover, the toxicity for each of the most active compounds was also assessed.