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Title: Cyclooctadiene Ru(II) complexes of thiophene-2-carboxaldehyde-derived thiosemicarbazones: synthesis, characterization and antiamoebic activity
Authors: Singh S.
Athar F.
Maurya, Mannar Ram
Azam A.
Published in: European Journal of Medicinal Chemistry
Abstract: Thiosemicarbazones (TSC) 1-10 were synthesized by condensing substituted thiosemicarbazide with thiophene-2-carboxaldehyde. These thiosemicarbazones were further reacted with [Ru(η4 -C8H12)(CH3CN)2Cl2] to form complexes of the type [Ru(η4 -C8H12)(TSC)Cl2] 1a-10a. Thiosemicarbazones exhibited antiamoebic activity in the range IC50 = 1.09-5.42 μM. In vitro assessment of antiamoebic activity indicated that the thiosemicarbazones 3, IC50 = 1.67 μM, 4, IC50 = 1.11 μM and 6, IC50 = 1.09 μM showed substantially less IC50 value than metronidazole (IC50 = 1.87 μM), a commonly used drug against amoebiasis. Cyclooctadiene Ru(II) complexes of thiosemicarbazones showed significant improvement in antiamoebic activity (IC50 = 0.30-1.39 μM). 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 μM of 4a and IC50 = 0.30 μM of 6a versus metronidazole). © 2006 Elsevier SAS. All rights reserved.
Citation: European Journal of Medicinal Chemistry, 41(5): 592-598
Issue Date: 2006
Keywords: Antiamoebic activity
Entamoeba histolytica.
Ru(II) Complexes
ISSN: 2235234
Author Scopus IDs: 22635972200
Author Affiliations: Singh, S., Department of Chemistry, Jamia Millia Islamia, Jamia Nagar, New Delhi, 110025, India
Athar, F., Department of Chemistry, Jamia Millia Islamia, Jamia Nagar, New Delhi, 110025, India
Maurya, M.R., Department of Chemistry, Indian Institute of Technology Roorkee, Roorkee, 247667, India
Azam, A., Department of Chemistry, Jamia Millia Islamia, Jamia Nagar, New Delhi, 110025, India
Funding Details: This work was supported from Council of Scientific and Industrial Research (Grant no. 27(0117)/02/EMR-ll), New Delhi, India. Council of Scientific and Industrial Research, India, CSIR: 27(0117)/02/EMR-ll
Corresponding Author: Azam, A.; Department of Chemistry, Jamia Nagar, New Delhi, 110025, India; email:
Appears in Collections:Journal Publications [CY]

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