Abstract A class of small molecules, thiosemicarbazones and derivatives have been studied over the last few years due to their wide pharmacological versatility. Due to having this wide-spectrum biological activity, interest on these compounds has been considerably increased in the pharmaceutical sector at the present time. Here, benzaldehyde and derivatives were used on N(4)-phenyl-3-thiosemicarbazide with glacial acetic acid to synthesize four thiosemicarbazones corresponding (1-4) in good yields (64-85%). Structures of compounds were characterized by spectrometric alanalysis: FT-IR, NMR 1H & 13C and MS spectra. A theoretical study based on their chemical structure has been made. In vitro antiparasitic activity of products has been evaluated on the on the bloodstream form of the strain 427 of Trypanosoma bruceibrucei. All compounds presented physical properties compatible with reasonable pharmacokinetics and drug availability, but they showed a low half inhibitory concentration (IC50> 100 µM) and then were not actives on the trypanosomes tested. Other biological activity would be explored on other pathogens.
Keywords Synthesis, N(4)-phenyl-3-thiosemicarbazones, reasonable pharmacokinetics.