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Abstract

Synthesis of 1,2,6-Thiadiazin 1,1-Dioxide Derivatives as Trypanocidal Agents

1
Cátedra de Química Orgánica, Facultad de Química, Universidad de la República General Flores 2124, Montevideo, Uruguay
2
Instituto de Química Médica (C.S.I.C.), Madrid, Spain
3
Departamento de Parasitología, Facultad de Farmacia, Universidad Complutense, Madrid, Spain
Molecules 2000, 5(3), 499-500; https://doi.org/10.3390/50300499
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 00499 i001
All the compounds were prepared according to the following synthetic pathway Molecules 05 00499 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

  1. 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.
  2. 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.; Di Maio, R.; Seoane, G.; Ochoa, C.; Gómez-Barrio, A.; Muelas, S. Synthesis of 1,2,6-Thiadiazin 1,1-Dioxide Derivatives as Trypanocidal Agents. Molecules 2000, 5, 499-500. https://doi.org/10.3390/50300499

AMA Style

Cerecetto H, Di Maio R, Seoane G, Ochoa C, Gómez-Barrio A, Muelas S. Synthesis of 1,2,6-Thiadiazin 1,1-Dioxide Derivatives as Trypanocidal Agents. Molecules. 2000; 5(3):499-500. https://doi.org/10.3390/50300499

Chicago/Turabian Style

Cerecetto, H., R. Di Maio, G. Seoane, C. Ochoa, A. Gómez-Barrio, and S. Muelas. 2000. "Synthesis of 1,2,6-Thiadiazin 1,1-Dioxide Derivatives as Trypanocidal Agents" Molecules 5, no. 3: 499-500. https://doi.org/10.3390/50300499

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