Abstract
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, 1H- and 13C-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.
Highlights
Tuberculosis (TB) is a widely spread respiratory disease which caused 1.3 million deaths worldwide in 2012 [1]
The certified dried and powdered aerial parts of Mikania glomerata were purchased from the Brazilian company called “Nutri Comércio de Ervas LTDA”, based on the city of São Paulo—SP
The extraction was performed as described in experimental section and the obtained kaurenoic acid (1) was identified by NMR experiments
Summary
Tuberculosis (TB) is a widely spread respiratory disease which caused 1.3 million deaths worldwide in 2012 [1]. It is considered the second leading cause of death from a single infectious agent, after HIV [1]. TB is a bacterial respiratory illness, caused by Micobacterium tuberculosis [2] It is contagious and airborne, which makes it somewhat difficult to avoid or to control. This disease mostly affects the lungs, causing coughing, and later leading to chest pains, weakness, weight loss and fever [2].
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