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Title: Cyclooctadiene Ru(II) complexes of thiophene-2-carboxaldehyde-derived thiosemicarbazones: synthesis, characterization and antiamoebic activity. Author: Singh S, Athar F, Maurya MR, Azam A. Journal: Eur J Med Chem; 2006 May; 41(5):592-8. PubMed ID: 16545496. Abstract: Thiosemicarbazones (TSC) 1-10 were synthesized by condensing substituted thiosemicarbazide with thiophene-2-carboxaldehyde. These thiosemicarbazones were further reacted with [Ru(eta4-C8H12)(CH3CN)2Cl2] to form complexes of the type [Ru(eta4-C8H12)(TSC)Cl2] 1a-10a. Thiosemicarbazones exhibited antiamoebic activity in the range IC50=1.09-5.42 microM. In vitro assessment of antiamoebic activity indicated that the thiosemicarbazones 3, IC50=1.67 microM, 4, IC50=1.11 microM and 6, IC50=1.09 microM showed substantially less IC50 value than metronidazole (IC50=1.87 microM), a commonly used drug against amoebiasis. Cyclooctadiene Ru(II) complexes of thiosemicarbazones showed significant improvement in antiamoebic activity (IC50=0.30-1.39 microM). All the complexes possess noteworthy potencies and showed less IC50 values than metronidazole against HK-9 strain of Entamoeba histolytica. Among all the complexes, the most promising antiamoebic activities was shown by the complexes 4a and 6a (IC50=0.31 microM of 4a and IC50=0.30 microM of 6a versus metronidazole).[Abstract] [Full Text] [Related] [New Search]