Synthesis and tripanocidal activity of ferrocenyl and benzyl diamines against Trypanosoma brucei and Trypanosoma cruzi
摘要:
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. (c) 2014 Elsevier Ltd. All rights reserved.
FUNCTIONALIZATION OF 1-AMINO-1-ARYLMETHYL PHOSPHONIC ACID DIETHYL ESTERS AT THE NH GROUP
作者:Salvatore Failla、Paolo Finocchiaro、Giorgio La Rosa
DOI:10.1080/10426509608046392
日期:1996.6.1
Functionalization at the NH group (s) of 1-amino-1-arylmethyl phosphonic acid diethyl esters with mono-isocyanates was performed in order to produce alkyl ureas bearing the phosphonate group. The condensation reaction is easily performed in dry toluene at 80 degrees C using a catalytic amount of Et(3)N, and the white crystalline products are obtained in satisfactory yields. Characterizations of these new compounds, of potential applications in agrochemistry, were performed by H-1-NMR spectroscopy and by MS-FAB spectrometry, which reveals the presence of very diagnostic signals or peaks for structural assignments.