Synthesis and in vitro anti-leishmanial activity of 1-(5-(5-nitrofuran-2-yl)-1,3,4-thiadiazol-2-yl)- and 1-(5-(5-nitrothiophen-2-yl)-1,3,4-thiadiazol-2-yl)-4-aroylpiperazines.

摘要

The synthesis and anti-leishmanial activity of nitroheteroaryl-1,3,4-thiadiazole-based compounds including 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 were described. Most of the synthesized compounds exhibited potent anti-leishmanial activity against both promastigote and amastigote forms of Leishmania major at non-cytotoxic concentrations. In general, 5-nitrofuran derivatives were more active than the corresponding 5-nitrothiophene analogues.