10.1016/j.bmc.2008.02.052
The research focuses on the synthesis and in vitro anti-leishmanial activity of nitroheteroaryl-1,3,4-thiadiazole-based compounds, specifically 1-[5-(5-nitrofuran-2-yl)-1,3,4-thiadiazol-2-yl]-4-aroylpiperazines and 1-[5-(5-nitrothiophen-2-yl)-1,3,4-thiadiazol-2-yl]-4-aroylpiperazines. The study involves the synthesis of these compounds using reactants such as 5-nitro-2-arylidene diacetates, thiosemicarbazide, ammonium ferric sulfate, and various aroyl chlorides. The synthesized compounds were then tested for their anti-leishmanial activity against both promastigote and amastigote forms of Leishmania major. The experiments utilized MTT assay to determine the IC50 values, which indicate the potency of the compounds. The analysis included the calculation of the logarithm of the partition coefficient (LogP) to assess the lipophilicity of the compounds, which is an important factor in their biological activity. The results showed that most of the synthesized compounds exhibited potent anti-leishmanial activity at non-cytotoxic concentrations, with 5-nitrofuran derivatives generally being more active than the corresponding 5-nitrothiophene analogues.
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