Antitrypanosomal activity of 5-nitro-2-aminothiazole-based compounds
179 - 186 (8)
European Journal of Medicinal Chemistry
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A small series of 5-nitro-2-aminothiazole-based amides containing arylpiperazine-, biphenyl- or aryloxyphenyl groups in their core were synthesized and evaluated as anti-trypanosomatid agents. All tested compounds were active or moderately active against Trypanosoma cruzi amastigotes in infected L6 cells and Trypanosoma brucei brucei, four were moderately active against Leishmania donovani axenic parasites while none were deemed active against Trypanosoma brucei rhodesiense. For the most active/moderately active compounds a moderate selectivity against the human infectious parasites was observed. There was a good correlation between lipophilicity (clogP value) versus antileishmanial activity and mammalian cell toxicity with a similar correlation also noted between clogP values and IC50 values against T. cruzi in structurally related subgroups of compounds. Three compounds were more potent as antichagasic agents than benznidazole.