Synthesis, spectrometric characterization and trypanocidal activity of some 1,3,4-thiadiazolines derivatives

Fatondji, Houssou Raymond;Gbaguidi, Fernand;Kpoviessii, Salomé;Bero, Joanne;Accrombessi, Georges Coffi;et.al.
(2010) International Journal of Biological and Chemical Sciences — Vol. 4, n° 6, p. 820-824 (2010)

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Authors
  • Fatondji, Houssou Raymond
    Author
  • Gbaguidi, Fernand
    Author
  • Kpoviessii, Salomé
    Author
  • Bero, JoanneUCLouvain
    Author
  • Hannaert, VéroniqueUCLouvain
    Author
  • Poupaert, JacquesUCLouvain
    Author
  • Accrombessi, Georges Coffi
    Author
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Abstract
Six 1,3,4-thiadiazolines derivatives were synthesized by cyclization of thiosemicarbazones under acetylating condition with yields going from 27 to 94%. The products purity was confirmed by LC/MS (Mass Spectrometry Coupled with High-Performance Liquid Chromatography) and they were characterized using spectrometry IR, NMR 1H and 13C (Nuclear Magnetic Resonance). These compounds were then tested in vitro on Trypanosoma brucei brucei according to the “LILIT, Alamar Blue” method to estimate their trypanocidal activity. 1,3,4-thiadiazoline 6 (IC50 = 38,79 ìM) was the most active of all compounds.
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Fatondji, H. R., Gbaguidi, F., Kpoviessii, S., Bero, J., Hannaert, V., Quetin-Leclercq, J., Poupaert, J., Moudachirou, M., & Accrombessi, G. C. (2010). Synthesis, spectrometric characterization and trypanocidal activity of some 1,3,4-thiadiazolines derivatives. International Journal of Biological and Chemical Sciences, 4(6), 820-824. https://doi.org/10.4314/ijbcs.v4i6.64982 (Original work published 2010)