title: Thiosemicarbazone fragment embedded within 1,2,4-triazole ring as inhibitors of Entamoeba histolytica.
abstract: A series of 1,2,4-triazole derivatives containing thiosemicarbazone linkage was synthesized and evaluated for their in vitro antiamoebic activity against HM1:IMSS strain of Entamoeba histolytica. All the compounds were capable of inhibiting the growth of E. histolytica out of which four compounds (IC(50)=0.28-1.38 μM) were found to have better efficacy than the standard drug Metronidazole (IC(50)=1.8 μM). Cytotoxicity of the active compounds was assessed by MTT assay using human breast cancer MCF-7 cell line, which revealed that all the compounds were low cytotoxic in the concentration range of 2.5-250 μM.
authors.affiliation: Department of Chemistry, Jamia Millia Islamia, Jamia Nagar, New Delhi, India.
authors.forename: Shadab Miyan
authors.initials: SM
authors.lastname: Siddiqui
authors.forename: Attar
authors.initials: A
authors.lastname: Salahuddin
authors.forename: Amir
authors.initials: A
authors.lastname: Azam
mesh_terms: D000981:Antiprotozoal Agents / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D004748:Entamoeba histolytica / Q000187:drug effects*; D005260:Female; D006801:Humans; D020128:Inhibitory Concentration 50; D008795:Metronidazole / Q000494:pharmacology; D015394:Molecular Structure; D013882:Thiosemicarbazones / Q000737:chemistry* / Q000494:pharmacology; D014230:Triazoles / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D000981:Antiprotozoal Agents; D013882:Thiosemicarbazones; D014230:Triazoles; D008795:Metronidazole