Synthesis of bicyclic 1,4-thiazepines as novel anti-Trypanosoma brucei brucei agents

Author:

Vairoletti Franco12345ORCID,Medeiros Andrea67589,Fontán Pablo12345,Meléndrez Jennifer12345,Tabárez Carlos12345,Salinas Gustavo10111258ORCID,Franco Jaime6758,Comini Marcelo A.6758ORCID,Saldaña Jenny1314345,Jancik Vojtech151617ORCID,Mahler Graciela12345ORCID,Saiz Cecilia12345ORCID

Affiliation:

1. Laboratorio de Química Farmacéutica

2. Departamento de Química Orgánica

3. Facultad de Química

4. Universidad de la República

5. Montevideo

6. Group Redox Biology of Trypanosomes

7. Institut Pasteur de Montevideo

8. Uruguay

9. Departamento de Bioquímica

10. Worm Biology Laboratory

11. Unidad Mixta Institut Pasteur de Montevideo-Facultad de Química

12. UdelaR

13. Laboratorio de Experimentación Animal

14. Depto de Ciencias Farmacéuticas

15. Centro Conjunto de Investigación en Química Sustentable UAEM-UNAM

16. Toluca

17. Mexico

Abstract

Bicyclic thiazolidinyl-1,4-thiazepines were prepared and evaluated as potential antiparasitic agents. We found thiazepines with low micromolar EC50 against T. b. brucei and high selectivity index.

Funder

Agencia Nacional de Investigación e Innovación

Comisión Sectorial de Investigación Científica

Publisher

Royal Society of Chemistry (RSC)

Subject

Pharmaceutical Science,Biochemistry,Drug Discovery,Molecular Medicine,Pharmacology,Organic Chemistry

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