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Title: Copper(II) complexes with substituted thiosemicarbazones of thiophene-2-carboxaldehyde: Synthesis, characterization and antiamoebic activity against E. histolytica
Authors: Sharma S.
Athar F.
Maurya, Mannar Ram
Azam A.
Published in: European Journal of Medicinal Chemistry
Abstract: In an effort to develop potent antiamoebic agents, a series of thiosemicarbazone (TSC) ligands 1-5 derived from thiophene-2-carboxaldehyde and N4-substituted thiosemicarbazides has been prepared and characterized using various spectroscopic techniques. Treatment of the ligands with cupric chloride produced the copper(II) complexes [Cu(TSC)2Cl2] 1a-5a where ligand bind through thionic sulfur and the azomethine nitrogen. The possible geometries of the complexes were assigned on the basis of magnetic moment, electronic and thermal patterns as well as infrared spectral studies. The thiosemicarbazones and their copper complexes were tested for their in vitro antiamoebic activity against HK-9 strain of Entamoeba histolytica and showed significant growth inhibition. The results revealed that these complexes are effective chemicals in inhibiting amoebal growth, with compound 5 (having -N(CH3)(C6H5) substituent at N4) and complexes 1a-5a being more effective than the commercial antiamoebic drug, metronidazole, based on IC50 values. These data also indicated that the compounds 3a and 5a are most effective among the complexes studied (IC 50 = 0.26 μM of 3a and IC50 = 0.21 μM of 5a versus IC50 = 1.81 μM of metronidazole). © 2005 Elsevier SAS. All rights reserved.
Citation: European Journal of Medicinal Chemistry, 40(12): 1414-1419
Issue Date: 2005
Keywords: Antiamoebic activity
Copper(II) complexes
ISSN: 2235234
Author Scopus IDs: 55491671400
Author Affiliations: Sharma, 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 by Council of Scientific and Industrial Research (Grant no. 27(0117)/02/EMR-II), New Delhi, India. The authors are thankful to Professor Alok Bhattacharya and Dr. Sudha Bhattacharya, School of Life Sciences and School of Environmental Sciences, Jawaharlal Nehru University, New Delhi, respectively, for providing Laboratory facilities for biological activities. Bangladesh Council of Scientific and Industrial Research, BCSIR: 27(0117)/02/EMR-II
Corresponding Author: Azam, A.; Department of Chemistry, Jamia Nagar, New Delhi 110025, India; email:
Appears in Collections:Journal Publications [CY]

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