851288-86-3Relevant academic research and scientific papers
Novel 3-nitrotriazole-based amides and carbinols as bifunctional antichagasic agents
Papadopoulou, Maria V.,Bloomer, William D.,Lepesheva, Galina I.,Rosenzweig, Howard S.,Kaiser, Marcel,Aguilera-Venegas, Benjamín,Wilkinson, Shane R.,Chatelain, Eric,Ioset, Jean-Robert
, p. 1307 - 1319 (2015)
3-Nitro-1H-1,2,4-triazole-based amides with a linear, rigid core and 3-nitrotriazole-based fluconazole analogues were synthesized as dual functioning antitrypanosomal agents. Such compounds are excellent substrates for type I nitroreductase (NTR) located in the mitochondrion of trypanosomatids and, at the same time, act as inhibitors of the sterol 14α-demethylase (T. cruzi CYP51) enzyme. Because combination treatments against parasites are often superior to monotherapy, we believe that this emerging class of bifunctional compounds may introduce a new generation of antitrypanosomal drugs. In the present work, the synthesis and in vitro and in vivo evaluation of such compounds is discussed.
