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TATAR, ESRA

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TATAR

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2013 - 20193
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Has files: false × Subject: Acylhydrazones ×

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    Synthesis, and prediction of molecular properties and antimicrobial activity of some acylhydrazones derived from N-(arylsulfonyl)methionine
    (SCIENTIFIC TECHNICAL RESEARCH COUNCIL TURKEY-TUBITAK, 2016) TATAR, ESRA; Tatar, Esra; Senkardes, Sevil; Sellitepe, Hasan Erdinc; Kucukguzel, Sukriye Guniz; Karaoglu, Sengul Alpay; Bozdeveci, Arif; De Clercq, Erik; Pannecouque, Christophe; Ben Hadda, Taibi; Kucukguzel, Ilkay
    A series of 38 new acylhydrazones [3-40], derived from (2S)-4-(methylsulfanyl)-2-[[(4-methylphenyl)sulfonyl] amino]butanoic acid hydrazide [2], were synthesized and evaluated for their anti-HIV and antimicrobial activity with the further aim to develop acylhydrazones carrying an amino acid side chain. All tested compounds possess stronger activity against gram (+) bacteria. Compound 23 was found active against methicillin-resistant Staphylococcus aureus (MRSA) with a MIC value of 3.9 mu g/mL. The MIC value of compound 30 against Enterococcus faecalis, Listeria monocytogenes, and Bacillus cereus was 8 mu g/mL. A computational study for prediction of ADME and drug-like properties (solubility, drug-likeness, and drug score) as well as potential toxicity profiles of compounds 2-40 was performed using the Molinspiration online property calculation toolkit and Osiris Property Explorer. As most of our compounds meet Lipinski's rule of five, they promise good solubility and permeability. According to Osiris calculations, the majority of our compounds are supposed to be nonmutagenic and nonirritating.
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    Synthesis and Biological Activity of N-(arylsulfonyl) Valine Hydrazones and Assistance of NMR Spectroscopy for Definitive 3D Structure
    (BENTHAM SCIENCE PUBL LTD, 2019) TATAR, ESRA; Senkardes, Sevil; Tatar, Esra; Nepravishta, Ridvan; Cela, Dorisa; Paci, Maurizio; Ozakpinar, Ozlem Bingol; Sekerler, Turgut; De Clercq, Erik; Pannecouque, Christophe; Kucukguzel, S. Guniz; Kucukguzel, Ilkay
    Background: Hydrazide-hydrazones constitute an important class of compounds for new drug development. In this study, a series of 39 new acylhydrazones (3-41), derived from (2S)-3-methyl-2-[[( 4-methylphenyl)sulfonyl]amino]butanoic acid hydrazide were synthesized with further aim to achieve biologically active acylhydrazones carrying an amino acid side chain. Methods: Compounds 3-41 were synthesized by microwave-assisted method. All synthesized compounds have been tested for their anti-HIV activity compound 21 was subjected to a new set of 2D-NMR analysis for the characterization of the isomers in solution and determination of its 3D structure. Results: The IC50 values for compounds 2-40 were found between >125-10.90 mu g/ml against HIV-1( IIIB) and HIV-2(ROD) strains in MT-4 cells. Compounds 3, 6, 10, 12, 23, 24, 27, 32, and 37 with CC50 values between 10.90-14.50 mu g/ml were selected to evaluate for their antileukemia activity. IC50 values for these mentioned compounds were found as >100 mu M on human chronic myelogenous leukemia, K562 cell line. Conclusion: Some compounds with IC50 values between 10.90-14.50 mu g/ml will be of benefit in the development of novel leads.
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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.