Synthesis, Spectrometrical Characterization and Pharmacological Properties of Six Substituted Hydrazones with Carbonyl Compounds
Bénédicta Kpadonou Kpoviessi
Laboratory of Physic and Synthesis Organic Chemistry (LaCOPS), Faculty of Sciences and Technics (FAST), University of Abomey-Calavi (UAC), 01 BP: 4166 Cotonou, Benin and Louvain Drug Research Institute (LDRI), School of Pharmacy, Université Catholique de Louvain, B1 7203 Avenue Emmanuel Mounier 72, B-1200 Brussels, Belgique.
Bardieu Atchadé
Laboratory of Physic and Synthesis Organic Chemistry (LaCOPS), Faculty of Sciences and Technics (FAST), University of Abomey-Calavi (UAC), 01 BP: 4166 Cotonou, Benin.
Basile Goueti
Laboratory of Physic and Synthesis Organic Chemistry (LaCOPS), Faculty of Sciences and Technics (FAST), University of Abomey-Calavi (UAC), 01 BP: 4166 Cotonou, Benin.
Hyacinthe Agnimonhan
Laboratory of Physic and Synthesis Organic Chemistry (LaCOPS), Faculty of Sciences and Technics (FAST), University of Abomey-Calavi (UAC), 01 BP: 4166 Cotonou, Benin.
Bienvenu Glinma
Laboratory of Physic and Synthesis Organic Chemistry (LaCOPS), Faculty of Sciences and Technics (FAST), University of Abomey-Calavi (UAC), 01 BP: 4166 Cotonou, Benin.
Fernand Gbaguidi
Laboratory of Physic and Synthesis Organic Chemistry (LaCOPS), Faculty of Sciences and Technics (FAST), University of Abomey-Calavi (UAC), 01 BP: 4166 Cotonou, Benin.
Joanne Bero
Louvain Drug Research Institute (LDRI), School of Pharmacy, Université Catholique de Louvain, B1 7203 Avenue Emmanuel Mounier 72, B-1200 Brussels, Belgique.
Salomé Kpoviessi *
Laboratory of Physic and Synthesis Organic Chemistry (LaCOPS), Faculty of Sciences and Technics (FAST), University of Abomey-Calavi (UAC), 01 BP: 4166 Cotonou, Benin and Louvain Drug Research Institute (LDRI), School of Pharmacy, Université Catholique de Louvain, B1 7203 Avenue Emmanuel Mounier 72, B-1200 Brussels, Belgique.
*Author to whom correspondence should be addressed.
Abstract
Hydrazones are molecules that prevent the growth of several microbial and parasitic strains by inhibited the replication of DNA sequences due to their chelating properties of metal ions. They are well recognized for Antiparasitic, Antimicrobial, Antibacterial, Antiviral, Antitumoral, Antimalarial and Anticonvulsive activities. The aim of the current study is to synthesized novel substituted hydrazones of ketones and aromatic aldehydes and to study their antiparasitic activities against Trypanosoma brucei brucei parasite. Synthesized hydrazone derivatives have been confirmed by elemental analysis and HPLC method, SMHR, 1H and 13C NMR spectroscopy. Three hydrazones derivatives have been synthesized namely phenylhydrazones, 2,4-dinitrophenyl hydrazones and benzohydrazones. The antiparasitic properties of these molecules were evaluated on Trypanosoma brucei brucei. The derivatives from phenylhydrazones and benzohydrazones were showing more antiparasitic activity like benzophenone benzohydrazone (D3) and salicylaldehyde phenylhydrazone (B1) compounds, which exhibited moderate activity on Trypanosoma brucei brucei (IC50 = 19.49 μM; IC50 = 20.01 μM respectively). Cytotoxicity tests again the human noncancer fibroblast cell line (WI38) were carried out with selected synthesized compounds and it showed that the most compounds were active against Trypanosoma brucei brucei. As a result of these findings, hydrazones could be a promising route in the treatment of trypanosomiasis.
Keywords: Synthesis, hydrazones, characterization, selectivity, Trypanosoma