Mannich base derivatives of 1,3,4-oxadiazole: synthesis and screening against Entamoeba histolytica

作者：Siddiqui Shadab Miyan; Salahuddin Attar; Azam Amir^*

来源：Medicinal Chemistry Research, 2013, 22(3): 1313-1319.

DOI：10.1007/s00044-012-0108-9

• 1,3,4-Oxadiazole
• Mannich base
• Antiamoebic activity
• E. histolytica
• MTT assay

Mannich base derivatives of 5-(pyridine-4-yl)-1,3,4-oxadiazole-2-(3H)-thione with substituted piperazine were synthesized and characterized. In vitro antiamoebic activity was performed against HM1: IMSS strain of Entamoeba histolytica and the cytotoxicity of the compounds having IC50 value less than metronidazole was assessed by MTT assay on human breast cancer MCF-7 cell line. The results revealed that compounds 2, 3 and 5 were found to be better inhibitors of E. histolytica than the reference drug metronidazole and found low cytotoxic in the concentration range of 2.5-250 mu M. This study suggests the possibility of developing 1,3,4-oxadiazole analogues as potential drug candidates.

• 出版日期2013-3