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Antitrypanosomal Activity of Novel Benzaldehyde-Thiosemicarbazone Derivatives from Kaurenoic Acid (†)
A series of new thiosemicarbazones derived from natural diterpene kaurenoic acid were synthesized and tested against the epimastigote forms of Trypanosoma cruzi to evaluate their antitrypanosomal potential. Seven of the synthesized thiosemicarbazones were more active than kaurenoic acid with IC(50)...
| Autores principales: | , , , , , , , , |
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| Formato: | Online Artículo Texto |
| Lenguaje: | English |
| Publicado: |
MDPI
2011
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| Materias: | |
| Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6259918/ https://www.ncbi.nlm.nih.gov/pubmed/21270733 http://dx.doi.org/10.3390/molecules16021166 |
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| author | Haraguchi, Shirani K. Silva, Adriano A. Vidotti, Gentil J. dos Santos, Phercyles V. Garcia, Francielle P. Pedroso, Raissa B. Nakamura, Celso V. de Oliveira, Cecília M. A. da Silva, Cleuza C. |
| author_facet | Haraguchi, Shirani K. Silva, Adriano A. Vidotti, Gentil J. dos Santos, Phercyles V. Garcia, Francielle P. Pedroso, Raissa B. Nakamura, Celso V. de Oliveira, Cecília M. A. da Silva, Cleuza C. |
| author_sort | Haraguchi, Shirani K. |
| collection | PubMed |
| description | A series of new thiosemicarbazones derived from natural diterpene kaurenoic acid were synthesized and tested against the epimastigote forms of Trypanosoma cruzi to evaluate their antitrypanosomal potential. Seven of the synthesized thiosemicarbazones were more active than kaurenoic acid with IC(50) values between 2-24.0 μM. The o-nitro-benzaldehyde-thiosemicarbazone derivative was the most active compound with IC(50) of 2.0 μM. The results show that the structural modifications accomplished enhanced the antitrypanosomal activity of these compounds. Besides, the thiocyanate, thiosemicarbazide and the p- methyl, p-methoxy, p-dimethylamine, m-nitro and o-chlorobenzaldehyde-thiosemicarbazone derivatives displayed lower toxicity for LLMCK(2) cells than kaurenoic acid, exhibing an IC(50) of 59.5 μM. |
| format | Online Article Text |
| id | pubmed-6259918 |
| institution | National Center for Biotechnology Information |
| language | English |
| publishDate | 2011 |
| publisher | MDPI |
| record_format | MEDLINE/PubMed |
| spelling | pubmed-62599182018-12-20 Antitrypanosomal Activity of Novel Benzaldehyde-Thiosemicarbazone Derivatives from Kaurenoic Acid (†) Haraguchi, Shirani K. Silva, Adriano A. Vidotti, Gentil J. dos Santos, Phercyles V. Garcia, Francielle P. Pedroso, Raissa B. Nakamura, Celso V. de Oliveira, Cecília M. A. da Silva, Cleuza C. Molecules Article A series of new thiosemicarbazones derived from natural diterpene kaurenoic acid were synthesized and tested against the epimastigote forms of Trypanosoma cruzi to evaluate their antitrypanosomal potential. Seven of the synthesized thiosemicarbazones were more active than kaurenoic acid with IC(50) values between 2-24.0 μM. The o-nitro-benzaldehyde-thiosemicarbazone derivative was the most active compound with IC(50) of 2.0 μM. The results show that the structural modifications accomplished enhanced the antitrypanosomal activity of these compounds. Besides, the thiocyanate, thiosemicarbazide and the p- methyl, p-methoxy, p-dimethylamine, m-nitro and o-chlorobenzaldehyde-thiosemicarbazone derivatives displayed lower toxicity for LLMCK(2) cells than kaurenoic acid, exhibing an IC(50) of 59.5 μM. MDPI 2011-01-26 /pmc/articles/PMC6259918/ /pubmed/21270733 http://dx.doi.org/10.3390/molecules16021166 Text en © 2011 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/). |
| spellingShingle | Article Haraguchi, Shirani K. Silva, Adriano A. Vidotti, Gentil J. dos Santos, Phercyles V. Garcia, Francielle P. Pedroso, Raissa B. Nakamura, Celso V. de Oliveira, Cecília M. A. da Silva, Cleuza C. Antitrypanosomal Activity of Novel Benzaldehyde-Thiosemicarbazone Derivatives from Kaurenoic Acid (†) |
| title | Antitrypanosomal Activity of Novel Benzaldehyde-Thiosemicarbazone Derivatives from Kaurenoic Acid (†) |
| title_full | Antitrypanosomal Activity of Novel Benzaldehyde-Thiosemicarbazone Derivatives from Kaurenoic Acid (†) |
| title_fullStr | Antitrypanosomal Activity of Novel Benzaldehyde-Thiosemicarbazone Derivatives from Kaurenoic Acid (†) |
| title_full_unstemmed | Antitrypanosomal Activity of Novel Benzaldehyde-Thiosemicarbazone Derivatives from Kaurenoic Acid (†) |
| title_short | Antitrypanosomal Activity of Novel Benzaldehyde-Thiosemicarbazone Derivatives from Kaurenoic Acid (†) |
| title_sort | antitrypanosomal activity of novel benzaldehyde-thiosemicarbazone derivatives from kaurenoic acid (†) |
| topic | Article |
| url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6259918/ https://www.ncbi.nlm.nih.gov/pubmed/21270733 http://dx.doi.org/10.3390/molecules16021166 |
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