2-amino-5-(3-4-dimethoxyphenyl)-1-3-4-thiadiazole and Chagas-Disease

Basing on a library of thiadiazole derivatives showing anti-trypanosomatidic activity, we have considered the thiadiazoles opened forms and reaction intermediates, thiosemicarbazones, as compounds of interest for phenotypic screening against Trypanosoma brucei (Tb), intracellular amastigote form of Leishmania infantum (Li) and Trypanosoma cruzi (Tc). Similar compounds have already shown interesting activity against the same organisms. The compounds were particularly effective against T. brucei and T. cruzi. Among the 28 synthesized compounds, the best one was (E)-2-(4-((3.4-dichlorobenzyl)oxy)benzylidene) hydrazinecarbothioamide (A14) yielding a comparable anti-parasitic activity against the three parasitic species (TbEC

Topics: Antiprotozoal Agents; Chagas Disease; Dose-Response Relationship, Drug; Humans; Macrophages; Molecular Structure; Parasitic Sensitivity Tests; Structure-Activity Relationship; Thiosemicarbazones; Trypanosoma