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Bioorg Med Chem Lett ; 24(7): 1707-10, 2014 Apr 01.
Article in English | MEDLINE | ID: mdl-24630563

ABSTRACT

Trypanosoma brucei and Trypanosoma cruzi are the etiologic agents of sleeping sickness and Chagas disease, respectively, two of the 17 preventable tropical infectious diseases (NTD) which have been neglected by governments and organizations working in the health sector, as well as pharmaceutical industries. High toxicity and resistance are problems of the conventional drugs employed against trypanosomiasis, hence the need for the development of new drugs with trypanocidal activity. In this work we have evaluated the trypanocidal activity of a series of N1,N2-dibenzylethane-1,2-diamine hydrochlorides (benzyl diamines) and N1-benzyl,N2-methyferrocenylethane-1,2-diamine hydrochlorides (ferrocenyl diamines) against T. brucei and T. cruzi parasite strains. We show that incorporation of the ferrocenyl group into the benzyl diamines increases the trypanocidal activity. The molecules exhibit potential trypanocidal activity in vitro against all parasite strains. Cytotoxicity assay was also carried out to evaluate the toxicity in HepG2 cells.


Subject(s)
Benzyl Compounds/pharmacology , Diamines/pharmacology , Ferrous Compounds/pharmacology , Trypanocidal Agents/pharmacology , Trypanosoma brucei brucei/drug effects , Trypanosoma cruzi/drug effects , Benzyl Compounds/chemical synthesis , Benzyl Compounds/chemistry , Cell Survival/drug effects , Diamines/chemical synthesis , Diamines/chemistry , Dose-Response Relationship, Drug , Ferrous Compounds/chemical synthesis , Ferrous Compounds/chemistry , Hep G2 Cells , Humans , Metallocenes , Molecular Structure , Parasitic Sensitivity Tests , Structure-Activity Relationship , Trypanocidal Agents/chemical synthesis , Trypanocidal Agents/chemistry
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