Literature DB >> 16213728

Synthesis, spectral studies and in vitro assessment for antiamoebic activity of new cyclooctadiene ruthenium(II) complexes with 5-nitrothiophene-2-carboxaldehyde thiosemicarbazones.

Shailendra Singh1, Fareeda Athar, Amir Azam.   

Abstract

We report here the synthesis, characterization and in vitro antiamoebic activity of 5-nitrothiophene-2-carboxaldehyde thiosemicarbazones (TSC), 1-5, and their bidentate complexes [Ru(eta(4)-C(8)H(12))(TSC)Cl(2)] 1a-5a. The biological studies of these compounds were investigated against HK-9 strain of Entamoeba histolytica and the concentration causing 50% cell growth inhibition (IC(50)) was calculated in the micromolar range. The ligands exhibited antiamoebic activity in the range (2.05-5.29microM). Screening results indicated that the potencies of the compounds increased by the incorporation of ruthenium(II) in the thiosemicarbazones. The complexes 1a-5a showed antiamoebic activity with an IC(50) of 0.61-1.43microM and were better inhibitors of growth of E. histolytica, based on IC(50) values. The most promising among them is Ru(II) complex 2a having 1,2,3,4-tetrahydroquinoline as N(4) substitution.

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Year:  2005        PMID: 16213728     DOI: 10.1016/j.bmcl.2005.08.103

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

Review 1.  Susceptibility Testing of Medically Important Parasites.

Authors:  Abebe Genetu Bayih; Anjan Debnath; Edward Mitre; Christopher D Huston; Benoît Laleu; Didier Leroy; Benjamin Blasco; Brice Campo; Timothy N C Wells; Paul A Willis; Peter Sjö; Wesley C Van Voorhis; Dylan R Pillai
Journal:  Clin Microbiol Rev       Date:  2017-07       Impact factor: 26.132

2.  Half-sandwich ruthenium–arene complexes with thiosemicarbazones: synthesis and biological evaluation of [(η⁶-p-cymene)Ru(piperonal thiosemicarbazones)Cl]Cl complexes.

Authors:  Floyd Beckford; Deidra Dourth; Michael Shaloski; Jacob Didion; Jeffrey Thessing; Jason Woods; Vernon Crowell; Nikolay Gerasimchuk; Antonio Gonzalez-Sarrías; Navindra P Seeram
Journal:  J Inorg Biochem       Date:  2011-08       Impact factor: 4.155

3.  A high-throughput drug screen for Entamoeba histolytica identifies a new lead and target.

Authors:  Anjan Debnath; Derek Parsonage; Rosa M Andrade; Chen He; Eduardo R Cobo; Ken Hirata; Steven Chen; Guillermina García-Rivera; Esther Orozco; Máximo B Martínez; Shamila S Gunatilleke; Amy M Barrios; Michelle R Arkin; Leslie B Poole; James H McKerrow; Sharon L Reed
Journal:  Nat Med       Date:  2012-06       Impact factor: 53.440

  3 in total

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