Synthesis and trypanocidal activity of novel pyridinyl-1,3,4-thiadiazole derivatives.

Biomedicine & Pharmacotherapy(2020)

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摘要
•New N-aminobenzyl or N-arylhydrazone 1,3,4-thiadiazole derivatives were synthesized.•Target compounds were designed as analogues of CYP51 inhibitors.•1,3,4-Thiadiazoles showed trypanocidal action in trypomastigote forms of T. cruzi.•Compound 11a produced phenotypic changes similar to those caused by posaconazole.•Hydrochloride 11a can be considered as a good trypanocidal drug candidate.
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关键词
Chagas disease,Trypanocidal activity,Inhibitor of sterol biosynthesis,2-amino-1,3,4-thiadiazole,1,3,4-thiadiazole-N-arylhydrazone
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