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TATAR, ESRA

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TATAR

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ESRA

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2013 - 20152
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    Novel 4-Thiazolidinones as Non-Nucleoside Inhibitors of Hepatitis C Virus NS5B RNA-Dependent RNA Polymerase
    (WILEY-V C H VERLAG GMBH, 2015) TATAR, ESRA; Cakir, Gizem; Kucukguzel, Ilkay; Guhamazumder, Rupa; Tatar, Esra; Manvar, Dinesh; Basu, Amartya; Patel, Bhargav A.; Zia, Javairia; Talele, Tanaji T.; Kaushik-Basu, Neerja
    In continuation of our efforts to develop new derivatives as hepatitis C virus (HCV) NS5B inhibitors, we synthesized novel 5-arylidene-4-thiazolidinones. The novel compounds 29-42, together with their synthetic precursors 22-28, were tested for HCV NS5B inhibitory activity; 12 of these compounds displayed IC50 values between 25.3 and 54.1 mu M. Compound 33, an arylidene derivative, was found to be the most active compound in this series with an IC50 value of 25.3 mu M. Molecular docking studies were performed on the thumb pocket-II of NS5B to postulate the binding mode for these compounds.
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    Some Hydrazones of 2-Aroylamino-3-methylbutanohydrazide: Synthesis, Molecular Modeling Studies, and Identification as Stereoselective Inhibitors of HIV-1
    (WILEY-V C H VERLAG GMBH, 2013) TATAR, ESRA; Tatar, Esra; Kucukguzel, Ilkay; Daelemans, Dirk; Talele, Tanaji T.; Kaushik-Basu, Neerja; De Clercq, Erik; Pannecouque, Christophe
    In accordance with our antiviral drug development attempt, acylhydrazone derivatives bearing amino acid side chains were synthesized for the evaluation of their antiviral activity against various types of viruses. Among these compounds, 8S, 11S, and 12S showed anti-HIV-1 activity with a 50% inhibitory concentration (IC50)=123.8 mu M (selectivity index, SI>3), IC50=12.1 mu M (SI>29), IC50=17.4 mu M (SI>19), respectively. Enantiomers 8R, 11R, and 12R were inactive against the HIV-1 strain IIIB. Hydrazones 8S, 11S, and 12S which were active against HIV-1 wild type showed no inhibition against a double mutant NNRTI-resistant strain (K103N;Y181C). Molecular docking calculations of R- and S-enantiomers of 8, 11, and 12 were performed using the hydrazone-bound novel site of HIV-1 RT.