Research Article | Volume : 2 Issue : 6, June 2012

Synthesis, characterization, anti-trypanosomal activity and toxicity against Artemia salinaLeach of thiobenzamides and derivatives

Finagnon H. Agnimonhan Leon Ahoussi Salome D. S. Kpoviessi Fernand A. Gbaguidi Coco N. Kapanda Joanne Bero Veronique Hannaert Joelle Quetin-Leclercq Mansourou Moudachirou Jacques Poupaert Georges C.Accrombessi   

Open Access    DOI: 10.7324/JAPS.2012.2601


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 µM) and 2 (IC50> 400 µM) have weak trypanocidal activities. However the larvae were sensitive to 2 (LD50 = 214 ± 9 µM) and therefore it could be used in cancer treatment.

Keyword:     Willgerodt-KindlerMontmorillonite K-10morpholin-4-yl (phenyl)-methanethione[4-(di-methylamino) phenyl] (morpholin-4-yl) methanethioneArtemia salina LeachtrypanocidalINTRODUCTION

Copyright:The Author(s). This is an open access article distributed under the Creative Commons Attribution Non-Commercial License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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