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[ Article ] Synthesis, characterization, purity verification, antiplasmodial activity and toxicity against Artemia salina Leach of salicylhydrazones and p-tosylhydrazones from S-(+)-carvone and arylketones

Date de soumission: 17-01-2017
Année de Publication: 2015
Entité/Laboratoire Laboratoires de Chimie Organique Phisyque et de Synthèse (LRCOPS)
Document type : Article
Discipline(s) : Chimie
Titre Synthesis, characterization, purity verification, antiplasmodial activity and toxicity against Artemia salina Leach of salicylhydrazones and p-tosylhydrazones from S-(+)-carvone and arylketones
Auteurs Atchade Bardieu [1], KPOVIESSI DOSSOU SIKA SALOME [2], Gbaguidi A. Fernand [3], GLINMA BIENVENU [4], Ahoussi Léon A. [5], GBENOU Joachim [6], Accrombessi Georges C. [7], Frederick Raphaël [8], Poupaert Jacques H. [9],
Journal: Journal of Chemical and Pharmaceutical Research
Catégorie Journal: Internationale
Impact factor: 0
Volume Journal: 7
DOI:
Resume Hydazones are molecules that inhibit the development of several microbes and parasites. They are known for their pharmacological activities: antimicrobial, antiviral, antitumor, antimalarial, Anticonvulsant. In this research, we synthesized with good yields(57-91%), substituted hydazones of 4'-methylacetophenone, 2-acetonaphthone, 7methoxy-1-tetralone andS (+)-carvone that formed two series: the series of salicylhydrazones(1a- 4a) and the series of p-tosylhydrazones of (1b-4b). Then we checked purity of molecules by elemental and HPLC analysis. Spectrometric analyzes methods such as HRMS, 1HNMR and 13C were used to confirm their structures. Their antiparasitic properties were evaluated on Plasmodium falciparum and the toxicity against Artemia salina Leach. Molecules of salicylhydrazones series presented moderate activity with good selectivity (7≤ SI ≤ 14). All compounds were found non-toxic to the larvae except 1a, 3b and 4b. In view of the observed activities and those already known, hydrazones could be a promising approach to the treatment of malaria.
Mots clés Synthesis, hydrazones, aryl ketone, purity, antiplasmodial activity, selectivity
Pages 318 - 326
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