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

Autor(es)

Matos, Priscilla M. ^[1] ; Mahoney, Brian ^[2] ; Chan, Yohan ^[2] ; Day, David P. ^[2] ; Cabral, Mirela M. W. ^[1] ; Martins, Carlos H. G. ^[1] ; Santos, Raquel A. ^[1] ; Bastos, Jairo K. ^[3] ; Page, Philip C. Bulman ^[2] ; Heleno, Vladimir C. G. ^[1]

Afiliação do(s) autor(es)

^[1] Univ Franca, Nucleo Pesquisas Ciencias Exatas & Tecnol, BR-14404600 Franca - Brazil

^[2] Univ E Anglia, Sch Chem, Norwich NR4 7TJ, Norfolk - England

^[3] Univ Sao Paulo, Fac Ciencias Farmaceut Ribeirao Preto, BR-14040903 Ribeirao Preto - Brazil

• Tipo de documento: Artigo Científico
• Fonte: Molecules; v. 20, n. 10, p. 18264-18278, OCT 2015.
• Citações Web of Science: 6

Resumo

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, H-1- and C-13-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. (AU)

• Processo FAPESP: 11/13630-7 - Validação química e farmacológica de extratos e princípios ativos de espécies de Copaifera
• Beneficiário: Jairo Kenupp Bastos
• Modalidade de apoio: Auxílio à Pesquisa - Temático
• Processo FAPESP: 09/09491-1 - Modificação estrutural e estudos detalhados por RMN de produtos naturais de interesse biológico
• Beneficiário: Vladimir Constantino Gomes Heleno
• Modalidade de apoio: Auxílio à Pesquisa - Regular