Reactivity Studies of 5,6-Dimethyl- and 3,5,6-Trimethyl -1,2,4-Triazine–N4-Oxide Against Different Electrophiles
Cátedra de Química Orgánica, Facultad de Química, Universidad de la República General Flores 2124, Montevideo, Uruguay
*
Author to whom correspondence should be addressed.
Molecules 2000, 5(3), 501-502; https://doi.org/10.3390/50300501
Published: 22 March 2000
Abstract
:It describes the synthesis of new 1,2,6-Thiadiazin 1,1-dioxide derivatives using condensation of the Knoevenagel type. The products are evaluated in vitro as trypanocidal agents.
Introduction
We have previously reported the synthesis of three series of new compounds and the biological evaluation against Trypanosoma cruzi of 1,2,6-Thiadiazin 1,1-dioxide derivatives, structurally related to Nifurtimox [1,2]. The in vitro assay showed that some of them exhibit significant activity against epimastigote forms of T. cruzi, but the cytotoxicity of this type of compounds against Vero cells was highest than the reference drug.
Experimental
In this work we design new structures, changing the free radical generator.
![Molecules 05 00501 i001]()
All the compounds were prepared according to the following synthetic pathway
![Molecules 05 00501 i002]()
Results and Discussion
All the compounds have been obtained with good yields, and have been characterized by IR, 1H-NMR, 13C-NMR and MS.
All the products were tested in vitro against T. cruzi epimastigote forms and that more promising were tested their cytotoxicity.
Acknowledgements
The authors thank CYTED (Ciencia y Tecnología para el desarrollo) and RELAQ (Red Latinoamericana de Ciencia Química).
References and Notes
- Synthesis and antichagasic properties of new 1,2,6-Thiadiazin-3,5-dione 1,1-dioxides, XVth INTERNATIONAL SYMPOSIUM ON MEDICINAL CHEMISTRY, 6 al 10 de setiembre de 1998, Edimburgo.
- Synthesis and antichagasic properties of new 1,2,6-Thiadiazin-3,5-dione 1,1-dioxides and related compounds. Arzneimittel Ferschung. (in press).
Share and Cite
MDPI and ACS Style
Cerecetto, H.; González, M.; Saenz, P.; Seoane, G. Reactivity Studies of 5,6-Dimethyl- and 3,5,6-Trimethyl -1,2,4-Triazine–N4-Oxide Against Different Electrophiles. Molecules 2000, 5, 501-502. https://doi.org/10.3390/50300501
AMA Style
Cerecetto H, González M, Saenz P, Seoane G. Reactivity Studies of 5,6-Dimethyl- and 3,5,6-Trimethyl -1,2,4-Triazine–N4-Oxide Against Different Electrophiles. Molecules. 2000; 5(3):501-502. https://doi.org/10.3390/50300501
Chicago/Turabian StyleCerecetto, H., M. González, P. Saenz, and G. Seoane. 2000. "Reactivity Studies of 5,6-Dimethyl- and 3,5,6-Trimethyl -1,2,4-Triazine–N4-Oxide Against Different Electrophiles" Molecules 5, no. 3: 501-502. https://doi.org/10.3390/50300501
