Synthesis, characterization, anti-trypanosomal activity and toxicity against Artemia salinaLeach of thiobenzamides and derivatives.
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Date
2012-06
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Abstract
This work aims to synthesize, characterize of thioamides benzaldehyde and 4-
(dimethylamino)benzaldehyde and assess their in votrotrypanocidal activity and totoxicity.
The Willgerodt-Kindler reaction preferred for the synthesis of thioamides morpholin-4-yl (phenyl)
methanethione 1 and [4 - (dimethylamino) phenyl] - (morpholin-4-yl) methanethione 2, is
catalyzed with montmorillonite K-10 and in a microwave oven. The structures of the thioamides
were characterized and confirmed by IR spectrometry, nuclear magnetic resonance (1H and 13C
NMR) and mass spectrometry (MS) Their trypanocidal activity was evaluated in the blood stream
form of the strain of Trypanosoma brucei brucei 427 using the "Lilit, Alamar Blue" (Baltz et al.,
1985; Hirumi et al., 1994; Räz et al., 1997) and cytotoxicity on brine shrimp larvae (Artemia
salina Leach) using the method of Michael et al. (1956) resumed by Vanhaecke et al. (1981) and
Sleet and Brendel (1983). The compounds1 (IC50> 483.09 M) and 2 (IC50> 400 M) have weak
trypanocidal activities. However the larvae were sensitive to 2 (LD50 = 214 ± 9 M) and therefore
it could be used in cancer treatment.
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Keywords
Willgerodt-Kindler, Montmorillonite K-10, morpholin-4-yl (phenyl)-methanethione, [4-(di-methylamino) phenyl] (morpholin-4-yl) methanethione, Artemia salina Leach, trypanocidal
Citation
Agnimonhan Finagnon H, Ahoussi Leon, Kpoviessi Salome D S, Gbaguidi Fernand A, Kapanda Coco N, Bero Joanne, Hannaert Veronique, Quetin-Leclercq Joelle, Moudachirou Mansourou, Poupaert Jacques, Accrombessi Georges C. Synthesis, characterization, anti-trypanosomal activity and toxicity against Artemia salinaLeach of thiobenzamides and derivatives. Journal of Applied Pharmaceutical Science. 2012 June; 2(6): 62-66.