Please use this identifier to cite or link to this item: http://dl.pgu.ac.ir/handle/10023/3359
Title: A class of 5-nitro-2-furancarboxylamides with potent trypanocidal activity against Trypanosoma brucei in vitro
Keywords: QD Chemistry;QD
Issue Date: 14-Feb-2013
Description: Recently, the World Health Organization approved the nifurtimox–eflornithine combination therapy for the treatment of human African trypanosomiasis, renewing interest in nitroheterocycle therapies for this and associated diseases. In this study, we have synthesized a series of novel 5-nitro-2-furancarboxylamides that show potent trypanocidal activity, 1000-fold more potent than nifurtimox against in vitro Trypanosoma brucei with very low cytotoxicity against human HeLa cells. More importantly, the most potent analogue showed very limited cross-resistance to nifurtimox-resistant cells and vice versa. This implies that our novel, relatively easy to synthesize and therefore cheap, 5-nitro-2-furancarboxylamides are targeting a different, but still essential, biochemical process to those targeted by nifurtimox or its metabolites in the parasites. The significant increase in potency (smaller dose probably required) has the potential for greatly reducing unwanted side effects and also reducing the likelihood of drug resistance. Collectively, these findings have important implications for the future therapeutic treatment of African sleeping sickness.;Publisher PDF;Peer reviewed
URI: http://europepmc.org/abstract/MED/23281892
http://dx.doi.org/10.1021/jm301215e
Other Identifiers: Zhou , L , Stewart , G , Rideau , E , Westwood , N J & Smith , T K 2013 , ' A class of 5-nitro-2-furancarboxylamides with potent trypanocidal activity against Trypanosoma brucei in vitro ' Journal of Medicinal Chemistry , vol 56 , no. 3 , pp. 796–806 . DOI: 10.1021/jm301215e
0022-2623
PURE: 45940624
PURE UUID: 859259e8-3c9e-465a-97ba-763f2081392e
PubMed: 23281892
Type Of Material: OTHER
Appears in Collections:Chemistry (School of)

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