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International Journal of Travel Medicine and Global Health، جلد ۷، شماره ۴، صفحات ۱۲۹-۱۳۴
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عنوان انگلیسی Halogenation as a Strategy to Improve Antiplasmodial Activity: A Report of New 3-Alkylpyridine Marine Alkaloid Analogs
چکیده انگلیسی مقاله Introduction: Due to the emergence of resistance to antimalarial drugs as well as the lack of vaccination for malaria, there is an urgent demand for the development of new antimalarial alternatives. Recently, our research group developed a new set of 3-alkylpyridine marine alkaloid analogs, of which a compound known as compound 5 was found to be inactive against Plasmodium falciparum. Methods: Herein, we report a successful halogenation strategy to improve the antiplasmodial activity of compound 5 through the replacement of a hydroxyl group by chlorine (compound 6) and fluorine (compound 7) atoms. Results: Compounds 6 and 7 showed improved antiplasmodial activities (IC50 = 7.2 and 8.3 μM, respectively) 20 times higher than that of their precursor, compound 5 (IC50 = 210.7 μM). Ultraviolet-visible titration experiments demonstrated that halogenation of compound 5 did not alter its ability to bind its target, hematin. Conclusion: Halogenation can enhance the antiplasmodial activity of a compound without altering its mechanism of action.
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نویسندگان مقاله Camila de Souza Barbosa |
Núcleo de Pesquisa em Química Biológica, Universidade Federal de São João Del-Rei, Campus Centro Oeste, Divinópolis, MG 35501-296, Brazil

Daniel Silqueira Martins Guimarães |
Instituto René Rachou, Fundação Oswaldo Cruz, Belo Horizonte, MG 30190-009, Brazil

Juliana da Costa Alves |
Núcleo de Pesquisa em Química Biológica, Universidade Federal de São João Del-Rei, Campus Centro Oeste, Divinópolis, MG 35501-296, Brazil

Cristiana Ferreira Alves de Brito |
Instituto René Rachou, Fundação Oswaldo Cruz, Belo Horizonte, MG 30190-009, Brazil

Renato Márcio Ribeiro-Viana |
Departamento Acadêmico de Química (DAQUI), Universidade Tecnológica Federal do Paraná, 86036-370 Londrina, Paraná, Brazil

Fernando de Pilla Varotti |
Núcleo de Pesquisa em Química Biológica, Universidade Federal de São João Del-Rei, Campus Centro Oeste, Divinópolis, MG 35501-296, Brazil

Gustavo Henrique Ribeiro Viana |
Núcleo de Pesquisa em Química Biológica, Universidade Federal de São João Del-Rei, Campus Centro Oeste, Divinópolis, MG 35501-296, Brazil

نشانی اینترنتی http://www.ijtmgh.com/article_99026_597db8b98dcb4ac2efac72b6a2a999b3.pdf
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