Novel 3-nitrotriazole-based amides and carbinols as bifunctional antichagasic agents.
Basic Information
ID: ALA3407483
Journal: J Med Chem
Title: Novel 3-nitrotriazole-based amides and carbinols as bifunctional antichagasic agents.
Authors: Papadopoulou MV, Bloomer WD, Lepesheva GI, Rosenzweig HS, Kaiser M, Aguilera-Venegas B, Wilkinson SR, Chatelain E, Ioset JR.
Abstract: 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.
CiteXplore: 25580906
DOI: 10.1021/jm5015742
Patent ID: ┄