Nitrotriazole-based acetamides and propanamides with broad spectrum antitrypanosomal activity.

ABSTRACT: 3-Nitro-1H-1,2,4-triazole-based acetamides bearing a biphenyl- or a phenoxyphenyl moiety have shown remarkable antichagasic activity both in vitro and in an acute murine model, as well as substantial in vitro antileishmanial activity but lacked activity against human African trypanosomiasis. We have shown now that by inserting a methylene group in the linkage to obtain the corresponding propanamides, both antichagasic and in particular anti-human African trypanosomiasis potency was increased. Therefore, IC50 values at low nM concentrations against both T. cruzi and T. b. rhodesiense, along with huge selectivity indices were obtained. Although several propanamides were active against Leishmania donovani, they were slightly less potent than their corresponding acetamides. There was a good co

SUBMITTER: Papadopoulou MV 

PROVIDER: S-EPMC5049494 | biostudies-literature | 2016 Nov

REPOSITORIES: biostudies-literature