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

Abstract

first_page settings Order Article Reprints Font Type: Arial Georgia Verdana Font Size: Aa Aa Aa Line Spacing:    Column Width:    Background: Open AccessAbstract Synthesis of 1,2,6-Thiadiazin 1,1-Dioxide Derivatives as Trypanocidal Agents by H. Cerecetto 1, R. Di Maio 1, G. Seoane 1, C. Ochoa 2, A. Gómez-Barrio 3 and S. Muelas 3 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 Download Download PDF Download PDF with Cover Download XML Download Epub Versions Notes 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. IntroductionWe 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. ExperimentalIn this work we design new structures, changing the free radical generator. All the compounds were prepared according to the following synthetic pathway Results and DiscussionAll 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 NotesSynthesis 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.; 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 Find Other Styles Article Metrics No No Article Access Statistics For more information on the journal statistics, click here. Multiple requests from the same IP address are counted as one view.