Synthesis and in vitro antifungal activity of new Mannich bases derived from 2-hydroxy-1,4-naphthoquinone (Lawsone)

Synthesis and in vitro antifungal activity of new Mannich bases derived from 2-hydroxy-1,4-naphthoquinone (Lawsone)

Allochio Filho, J. F.; Roldi, L. L.; Fiorot, R.; Greco, S. J.; Lacerda Jr., V.; dos Santos, R. B.; de Castro, E. V. R.; Ferreira, J. M. S.; Aleixo, A. A.; Carvalho, F. S.; Carvalho, R. S.

Abstract:

The fungal infection is the one of most very important problem that affects immunocompromised patients due to AIDS and cancer. Azoles are the most widely antifungal drugs acting on the inhibition of the 14α-demethylase enzyme, very important therapeutic target. Additionally, the generation of reactive oxygen species (ROS) is very important for antifungal activity and the naphthoquinones, as lawsone, are known compounds with higher capacity to generate ROS. In this work, we have been synthesized new enolaminas through multicomponent Mannich reaction in lawsone with various aldehydes and amines in ethanol and analyzed the synergy effect of triazole and the ROS.

The fungal infection is the one of most very important problem that affects immunocompromised patients due to AIDS and cancer. Azoles are the most widely antifungal drugs acting on the inhibition of the 14α-demethylase enzyme, very important therapeutic target. Additionally, the generation of reactive oxygen species (ROS) is very important for antifungal activity and the naphthoquinones, as lawsone, are known compounds with higher capacity to generate ROS. In this work, we have been synthesized new enolaminas through multicomponent Mannich reaction in lawsone with various aldehydes and amines in ethanol and analyzed the synergy effect of triazole and the ROS.

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DOI: 10.5151/chempro-15bmos-BMOS2013_2013916122532

Referências bibliográficas

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Como citar:

Allochio Filho, J. F.; Roldi, L. L.; Fiorot, R.; Greco, S. J.; Lacerda Jr., V.; dos Santos, R. B.; de Castro, E. V. R.; Ferreira, J. M. S.; Aleixo, A. A.; Carvalho, F. S.; Carvalho, R. S.; "Synthesis and in vitro antifungal activity of new Mannich bases derived from 2-hydroxy-1,4-naphthoquinone (Lawsone)", p-284-284. In: In Blucher Chemistry Proceedings, São Paulo, v. 1, n. 2, Dezembro.2013. São Paulo: Blucher, 2013.
ISSN 23184043, DOI 10.5151/chempro-15bmos-BMOS2013_2013916122532