Pentacyclic nitrofurans that rapidly kill nifurtimox-resistant trypanosomes

Abstract

Pentacyclic nitrofuran isoxazolines warrant further development for the treatment of drug-susceptible and nifurtimox-resistant trypanosome infections.

Current and Future Prospects of Nitro-compounds as Drugs for Trypanosomiasis and Leishmaniasis

“…In addition to that described above, a number of recent publications have reported numerous novel nitroaromatics which possess promising in vitro activity against one, or more kinetoplastid parasites (Figure 4) [79][80][81][82][83][84][85][86][87][88]. These and other studies have established that the anti-kinetoplastid nitroaromatic pharmacophore is not limited to just nitroimidazoles and nitrofurans, but encompasses a range of ring systems, including nitrothiazoles (e.g.…”

“…Nitrofurans IV and X have both been shown to be active against nifurtimox-resistant T. brucei, suggesting that their modes of action are at least in part divergent. [87]; II, compound 6 from [88]; III, compound 3m from [80]; IV, compound 15 from [79]; V, compound 6 from [81]; VI, compound 20 from [82]; VII, compound 2NB from [83]; VIII, compound 2 from [85]; IX, compound 3 from [84]; and X, compound 22s from [86].…”