title: Structural and antitrypanosomal data of different carbasones of piperitone.
abstract: This article reports data on four carbazones of piperitone: semicarbazone1, thiosemicarbazone2, 4-phenyl semicarbazone3and 4-phenyl thiosemicarbazone4prepared directlyin situfrom essential oil ofCymbopogon schoenantus,whose GC-FID and GC-MS analysis revealed piperitone as major component (68.20%). The structures of hemi-synthesized compounds were confirmed by high throughput IR, MS,1H and13C NMR based spectrometric analysis. Their antiparasitic activities were evaluatedin vitroonTrypanosoma brucei brucei(Tbb). The compound3(IC50=8.63±0.81 µM) and4(IC50=10.90±2.52 µM) exhibited antitrypanosomal activity,2had a moderate activity (IC50=74.58±4.44 µM) but1was void of significant activity (IC50=478.47 µM). Thein vitrotests showed that all compounds were less cytotoxic against the human non cancer fibroblast cell line (WI38) (IC50>80 µM) while only2(IC50=21.16±1.37 μM) and4(IC50=32.22±1.66 µM) were cytotoxic against the Chinese Hamster Ovary (CHO) cells and toxic onArtemia salina(Leach) larvae. Piperitone 4-phenyl semicarbazone3, the best antitrypanosomal compound, showed also a selectivity index (SI) higher than 7 on the larvae and the tested cells and therefore might be further studied as antitrypanosomal agent. Also, all compounds except3showed selectivity between the two tested cell lines (SI>2). This data reveals for the first time the antitrypinosomal properties of thiosemicarbazones, their cytotoxicity on mammalian cells as well as their activities againstTbbandA. salinaLeach.
authors.affiliation: University of Abomey-Calavi (UAC), Faculty of Sciences and Technics (FAST), Department of Chemistry, Laboratory of Physic and Synthesis Organic Chemistry (LaCOPS), 01 PB: 4521, Cotonou, Benin.
authors.forename: Amoussatou
authors.initials: A
authors.lastname: Sakirigui
authors.affiliation: University of Abomey-Calavi (UAC), Faculty of Sciences and Technics (FAST), Department of Chemistry, Laboratory of Physic and Synthesis Organic Chemistry (LaCOPS), 01 PB: 4521, Cotonou, Benin; Laboratoire de Pharmacognosie, Centre Béninois de Recherche Scientifique et Technique, 01 PB 06 Oganla, Porto-Novo, Benin.
authors.forename: Fernand
authors.initials: F
authors.lastname: Gbaguidi
authors.affiliation: Laboratoire de Chimie Pharmaceutique Organique, Faculté des Sciences de la Santé, Université d׳Abomey-Calavi, Campus du Champ de Foire, 01 BP 188, Cotonou, Bénin.
authors.forename: Urbain C
authors.initials: UC
authors.lastname: Kasséhin
authors.affiliation: Université catholique de Louvain (UCL), Louvain Drug Research Institute (LDRI), B1 7203 Av. E. Mounier 72, B-1200 Bruxelles, Belgium.
authors.forename: Jacques
authors.initials: J
authors.lastname: Poupaert
authors.affiliation: University of Abomey-Calavi (UAC), Faculty of Sciences and Technics (FAST), Department of Chemistry, Laboratory of Physic and Synthesis Organic Chemistry (LaCOPS), 01 PB: 4521, Cotonou, Benin.
authors.forename: Georges C
authors.initials: GC
authors.lastname: Accrombessi
authors.affiliation: Department of Biology, Rutgers University, 315 Penn St., Camden, NJ 08102, USA; Center for Computational and Integrative Biology, 315 Penn St., Camden, NJ 08102, USA.
authors.forename: Simeon O
authors.initials: SO
authors.lastname: Kotchoni
keywords: Artemia salina; Cymbopogon shoenantus; Essential oil; Hemi-synthesized; Piperitone carbazones; Trypanosoma brucei brucei