Person: TATAR, ESRA
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TATAR
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ESRA
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Publication Open Access Novel 1,2,4-triazoles derived from Ibuprofen: synthesis and in vitro evaluation of their mPGES-1 inhibitory and antiproliferative activity(2022-11-01) BİNGÖL ÖZAKPINAR, ÖZLEM; KULABAŞ, NECLA; TATAR, ESRA; KÜÇÜKGÜZEL, İLKAY; Bulbul B., Ding K., Zhan C., Ciftci G., YELEKÇİ K., Gurboga M., BİNGÖL ÖZAKPINAR Ö., Aydemir E., Baybag D., ŞAHİN F., et al.Some novel triazole-bearing ketone and oxime derivatives were synthesized from Ibuprofen. In vitro cytotoxic activities of all synthesized molecules against five cancer lines (human breast cancer MCF-7, human lung cancer A549, human prostate cancer PC-3, human cervix cancer HeLa, and human chronic myelogenous leukemia K562 cell lines) were evaluated by MTT assay. In addition, mouse embryonic fibroblast cells (NIH/3T3) were also evaluated to determine the selectivity. Compounds 18, 36, and 45 were found to be the most cytotoxic, and their IC50 values were in the range of 17.46-68.76 mu M, against the tested cancer cells. According to the results, compounds 7 and 13 demonstrated good anti-inflammatory activity against the microsomal enzyme prostaglandin E2 synthase-1 (mPGES-1) enzyme at IC50 values of 13.6 and 4.95 mu M. The low cytotoxicity and non-mutagenity of these compounds were found interesting. Also, these compounds significantly prevented tube formation in angiogenesis studies. In conclusion, the anti-inflammatory and angiogenesis inhibitory activities of these compounds without toxicity suggested that they may be promising agents in anti-inflammatory treatment and they may be supportive agents for the cancer treatment.Publication Metadata only Fabrication and characterisation studies of cyclodextrin-based nanosponges for sulfamethoxazole delivery(SPRINGER, 2020) TATAR, ESRA; Yasayan, Gokcen; Sert, Betul Satiroglu; Tatar, Esra; Kucukguzel, Ilkaybeta-Cyclodextrin based nanosponges have been synthesized in three molar ratios, and characterized by phase solubility studies, Fourier-transform infrared spectroscopy, matrix-assisted laser desorption/ionization time of flight mass spectrometry, and scanning electron microscopy. Following characterization studies, a model anti-bacterial agent, sulfamethoxazole, has been loaded within the nanosponges, and in vitro drug release studies were carried out. According to results, nanosponges below similar to 100 nm diameter were obtained with a characteristic sponge-like morphology. Phase solubility studies demonstrated that beta-cyclodextrin nanosponges improve solubility of the drug up to 30-fold. These results suggest that nanosponges could improve the bioavailability of drugs by conducing them to reach desired plasma concentrations for therapeutic effect. [GRAPHICS] .Publication Open Access A Comparison Study of Fiber Diameter's Effect on Characteristic Features of Donepezil/Curcumin-Loaded Polycaprolactone/Polylactic Acid Nanofibers(2022-05-01) EKENTOK ATICI, CEYDA; GÜNDÜZ, OĞUZHAN; ÇAM, MUHAMMET EMİN; TATAR, ESRA; YAVUZ, AYŞE NUR; Aydin S., Kabaoglu I., Guler E., Topal F., YAVUZ A. N., EKENTOK ATICI C., TATAR E., Gurbuz F., GÜNDÜZ O., ÇAM M. E.Nanofibers (NFs) offer an alternative option for the treatment of Alzheimer\"s disease (AD) by addressing unmet clinical problems. In this study, anti-AD drugs, donepezil (DO) and curcumin (CUR), are loaded in polylactic acid/polycaprolactone NFs. The effect of fiber diameter on drug release behavior is mainly observed, and the successful loading of DO and CUR to NFs is demonstrated. The tensile strength of DO/CUR-loaded NFs (DNFs) with lower fiber diameter is found to be higher. The working temperature is increased by the decrease of glass transition temperature and increase of the melting temperature after loading drugs. Furthermore, the increase in the percentage of swelling and decrease in the degradation rate for NFs are observed due to the increase of fiber diameter. Encapsulation efficiency and burst release percentages for DNFs are augmented by the increase of fiber diameter. Nevertheless, DNFs exhibit a sustained drug release manner over 2 weeks. NFs do not demonstrate a toxic effect on L929 (mouse fibroblast) cells, and additionally, they promote cell proliferation. Considering all these results, it is proven that the fiber diameter affects all characteristic features of NFs, and DNFs lead to a new and promising drug delivery system for the treatment of AD.Publication Open Access Oral empagliflozin-loaded tri-layer core-sheath fibers fabricated using tri-axial electrospinning: Enhanced in vitro and in vivo antidiabetic performance(2023-03-25) TATAR, ESRA; GÜNDÜZ, OĞUZHAN; Guler E., Nur Hazar-Yavuz A., TATAR E., Morid Haidari M., Sinemcan Ozcan G., DURUKSU G., Graça M. P. F., Kalaskar D. M., GÜNDÜZ O., Emin Cam M.Empagliflozin (EM) was successfully loaded in polycaprolactone/poly (L-lactic acid)/polymethyl methacrylate (PCL/PLA/PMMA) fibers. In the rat β-cell line (BRIN-BD11), the insulin expression ratio of pancreatic β-cells was stimulated at high and low glucose by culturing with tri-layer EM-loaded fiber (EMF) for 48 h. The expression ratios of glucokinase and GLUT-2 proteins increased after EMF treatment. According to the in vitro drug release test, 97% of all drug contained in fibers was released in a controlled manner for 24 h. The pharmacokinetic test revealed that the bioavailability was improved ∼4.8-fold with EMF treatment compared to EM-powder and blood glucose level was effectively controlled for 24 h with EMF. Oral administration of EMF exhibited a better sustainable anti-diabetic activity even in the half-dosage than EM-powder in streptozotocin/nicotinamide-induced T2DM rats. The levels of GLP-1, PPAR-γ, and insulin were increased while the levels of SGLT-2 and TNF-α were decreased with EMF treatment. Also, EMF recovered the histopathological changes in the liver, pancreas, and kidney in T2DM rats and protected pancreatic β-cells. Consequently, EMF is suggested as an unprecedented and promotive treatment approach for T2DM with a higher bioavailability and better antidiabetic effect compared to conventional dosage forms.Publication Open Access Synthesis, in vitro and in silico studies on novel 3-aryloxymethyl-5-[(2-oxo-2-arylethyl)sulfanyl]-1,2,4-triazoles and their oxime derivatives as potent inhibitors of mPGES-1(2023-01-01) KULABAŞ, NECLA; TATAR, ESRA; KÜÇÜKGÜZEL, İLKAY; BİNGÖL ÖZAKPINAR, ÖZLEM; Erensoy G., Ding K., Zhan C., Çiftçi G., Yelekçi K., Duracık M., Bingöl Özakpınar Ö., Aydemir E., Yılmaz Z. N. , Şahin F., et al.Human microsomal prostaglandin E synthase (mPGES)-1 is a glutathione-dependent membrane-bound enzyme which is involved in the terminal stage of prostaglandin E2 (PGE2) synthesis. It has been well reported as a key target for the discovery of new anti-inflammatory and anti-cancer drugs. Specific inhibitors of mPGES-1 are anticipated to selectively restrain the generation of PGE2 induced by the inflammatory stimuli, without obstructing of the regular biosynthesis of other homeostatic prostanoids. Therefore, the design of mPGES-1 inhibitors can represent a better choice to take control of PGE2 associated diseases, compared with conventional non-steroidal anti-inflammatory drugs and cyclooxygenase (COX) inhibitors, which are known for their serious side effects. Although there is an intensive effort for the identification of mPGES-1 inhibitors, none of the unveiled molecules so far have reached the clinical market. Therefore, the development of novel mPGES-1 inhibitors with proper drug-like properties is still an unmet medical need. As a continuation of our research for the identification of new chemotypes which might inhibit this enzyme, we now report the design and synthesis of 3-aryloxymethyl-5-[(2-oxo2-arylethyl)sulfanyl]-1,2,4-triazoles and their oxime derivatives as inhibitors of human mPGES-1. All synthesized compounds were characterized by FTIR, 1H NMR, 13C NMR (for compounds 12, 14, 15, 26, 27), HMBC (for compounds 6, 7, 8, 16, 19, 23, 28), and MS data. Twenty-four target compounds 7–30 were screened for their mPGES-1/COX-2 inhibitory activities as well as their cytotoxicity. Of these compounds, 20 and 24 showed potent mPGES-1 inhibition by IC50 values of 0.224±0.070 μM and 1.08±0.35 μM, respectively. These two compounds have also been observed to inhibit angiogenesis in matrigel tube formation assay with no toxicity toward HUVEC cells. In silico studies were also held to understand inhibition mechanisms of the most active compounds using molecular docking, molecular dynamics calculations and ADMET predictions.Publication Open Access Synthesis, characterization and biological evaluation of 1,3-thiazolidine-4-ones derived from (2S)-2-benzoylamino-3-methylbutanohydrazide hydrazones(MARMARA UNIV, 2021) TATAR, ESRA; Tatar, Esra; Kucukguzel, Ilkay; Otuk, Gulten; Bilgin, Merve; De Clercq, Erik; Andrei, Graciela; Snoeck, Robert; Pannecouque, Christophe; Kaushik-Basu, NeerjaNovel 2-aryl-5-non-substituted / methyl-1,3-thiazolidine-4-one derivatives 14-33 carrying L-valine core were synthesized by the reaction of acylhydrazones 4-13 with thioglycolic acid / thiolactic acid. Structures of all synthesized compounds 14-33 were confirmed by IR, H-1-NMR and HR-MS analysis and C-13-NMR were recorded for selected compounds 17, 21, 28 and 30. None of the compounds 14-33 showed activity against HIV-1 (strain IIIB) or HIV-2 (strain ROD) in an MT-4/MTT based assay. Compounds 14-33 were also screened against Feline Corona Virus (FIPV), Feline Herpes Virus, HSV-1(KOS), HSV-1 (TK-KOS ACVr), HSV-2 (G), Vaccinia virus, Vesicular stomatitis virus, Cytomegalovirus, Varicella-Zoster virus, Respiratory syncytial virus, Coxsackie B4 virus, Parainfluenza-3 virus, Reovirus-1, Sindbis virus and Punta Toro virus, but none of them showed antiviral activity at subtoxic concentrations. Anti-HCV NS5B RdRp activity of some selected compounds from the series 14-33 were found to vary between 4.1-27 % at the concentration of 100 mu M. In vitro antibacterial activity evaluation of selected compounds 16-23 and 25-32, against Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853, Enterococcus faecalis ATCC 29212, Klebsiella pneumoniae ATCC 4352, Bacillus subtilis ATCC 6633, Staphylococcus epidermidis ATCC 12228, MRSA and antifungal activity against Candida albicans ATCC 10231 resulted in the MIC values between 625->5000 mu g/ml.Publication Open Access Small-Molecule Inhibitors Targeting Sterol 14 alpha-Demethylase (CYP51): Synthesis, Molecular Modelling and Evaluation AgainstCandida albicans(WILEY-V C H VERLAG GMBH, 2020-07-20) TATAR, ESRA; Binjubair, Faizah A.; Parker, Josie E.; Warrilow, Andrew G.; Puri, Kalika; Braidley, Peter J.; Tatar, Esra; Kelly, Steven L.; Kelly, Diane E.; Simons, ClaireFungal infections are a global issue affecting over 150 million people worldwide annually, with 750 000 of these caused by invasiveCandidainfections. Azole drugs are the frontline treatment against fungal infections; however, resistance to current azole antifungals inC. albicansposes a threat to public health. Two series of novel azole derivatives, short and extended derivatives, have been designed, synthesised and investigated for CYP51 inhibitory activity, binding affinity and minimum inhibitory concentration (MIC) againstC. albicansstrains. The short derivatives were more potent against theC. albicansstrains (e. g., MIC 2-(4-chlorophenyl)-N-(2,4-dichlorobenzyl)-3-(1H-imidazol-1-yl)propanamide (5 f) <0.03 mu g/mL,N-(4-((4-chlorophenyl)sulfonamido)benzyl)-2-phenyl-3-(1H-1,2,4-triazol-1-yl)propanamide (12 c), 1 mu g/mL, fluconazole 0.125 mu g/mL) but both displayed comparable enzyme binding and inhibition (5 fK(d)62 +/- 17 nM, IC(50)0.46 mu M;12 cK(d)43 +/- 18 nM, IC(50)0.33 mu M, fluconazoleK(d)41 +/- 13 nM, IC(50)0.31 mu M, posaconazoleK(d)43 +/- 11 nM, IC(50)0.2 mu M). The short series had poor selectivity for CaCYP51 over the human homologue, whereas the selectivity of the extended series, for example, compound12 c, was higher (21.5-fold) than posaconazole (4.7-fold) based onK(d)values, although posaconazole was more selective (615-fold) than12 c(461-fold) based on IC(50)values. Based on inhibitory activity and selectivity profile, the extended series are the better of the two series for further development.