Person: KARAKUŞ, SEVGİ
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KARAKUŞ
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SEVGİ
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Publication Metadata only Synthesis, antiviral and anticancer activity of some novel thioureas derived from N-(4-nitro-2-phenoxyphenyl)-methanesulfonamide(ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER, 2009) KÜÇÜKGÜZEL, İLKAY; Karakus, Sevgi; Kucukguzel, S. Guniz; Kucukguzel, Ilkay; De Clercq, Erik; Pannecouque, Christophe; Andrei, Graciela; Snoeck, Robert; Sahin, Fikrettin; Bayrak, Oemer FarukDue to a continuing effort to develop new antiviral agents, a series of 1-[4-(methanesulfonamido)-3-phenoxyphenyl]-3-alkyl/aryl thioureas 3a-i have been synthesized by the reaction of alkyl/aryl isothiocyanates with 4-amino-2-phenoxymethanesulfonanilide. These derivatives were structurally characterized by the use of spectral techniques and evaluated for their anticancer and antiviral activities. None of the tested compounds showed significant anticancer properties on A549 and L929 cell lines. All synthesized compounds 3a-i were evaluated in vitro against HIV-1 (IIIB) and HIV-2 (ROD) strains in MT-4 cells, as well as other selected viruses such as HSV-1, HSV-2, Coxsackie virus B4, Sindbis virus and varicella-zoster virus using HEL, HeLa and Vero cell cultures. Compound 3b was able to block HIV replication with almost 100% maximum protection at 125 mu g/ml, and IC50 values of 54.9 mu g/ml and 65.9 mu g/ml against HIV-1 and HIV-2, respectively. (C) 2009 Elsevier Masson SAS. All rights reserved.Publication Metadata only Synthesis, anticancer evaluation and in silico ADMET studies on urea/thiourea derivatives from gabapentin(TAYLOR & FRANCIS LTD, 2020) KAYMAKÇIOĞLU, BEDİA; Turk, Sevda; Tok, Fatih; Erdogan, Omer; Cevik, Ozge; Tok, Tugba Taskin; Kocyigit-Kaymakcioglu, Bedia; Karakus, Sevgi2-(1-((3-Substitutedureido/thioureido)methyl)cyclohexyl)acetic acid derivatives (1-9) were synthesized from gabapentin. All the synthesized compounds were characterized by using IR, H-1-NMR, C-13-NMR spectroscopy, mass spectrometry and elemental analysis. Urea and thiourea derivatives were investigated for their potential in vitro anticancer activities on PC3 and MCF7 cancer cell lines using MTT assay. Cell apoptosis was detected by with Annexin V Assay. Our results showed that compound 8 {2-(1-((3-(2,6-dichlorophenyl)ureido)methyl)cyclohexyl)acetic acid} significantly inhibited the proliferation and growing of PC3 and MCF7 cells. Both cell types showed dysfunction of cellular morphology which induced apoptosis 10 mu M concentration of compound 8 treated cells. Our results indicate that compound 8 might have significance as an anti-tumor agent against human prostate and breast cancer. The theoretical structure and activity estimation via in silico ADMET was also examined.Publication Metadata only Synthesis, anticancer activity and ADMET studies of N-(5-methyl-1,3,4-thiadiazol-2-yl)-4-[(3-substituted)ureido/thioureido] benzenesulfonamide derivatives(TAYLOR & FRANCIS LTD, 2018) KAYMAKÇIOĞLU, BEDİA; Karakus, S.; Tok, F.; Tuerk, S.; Salva, E.; Tatar, G.; Taskin-Tok, T.; Kocyigit-Kaymakcioglu, B.A series of novel 4-[(3-substituted)ureido]-N-(5-methyl-1,3,4-thiadiazol-2-yl) benzenesulfonamides and 4-[(3-substituted)thioureido]-N-(5-methyl-1,3,4-thiadiazol-2-yl)benzenesulfonamides were prepared from 4-amino-N-(5-methyl-1,3,4-thiadiazol-2-yl)benzenesulfonamide (sulfamethizole). The structures of the synthesized compounds were determined by IR, H-1-NMR, MS and elemental analysis. The anticancer activity of these compounds was evaluated against human colorectal carcinoma (HCT116) and human cervix carcinoma (HeLa) cell lines. Compound 4 (4-{[(2,4-dichlorophenyl)carbamoyl]amino}-N-(5-methyl-1,3,4-thiadiazol-2-yl)benzenesulfonamide) showed marked anticancer activity, being the most active compounds in this series with the IC50 value of 13.92 +/- 0.22 mu M and 37.91 +/- 0.10 mu M against HeLa and HCT116, respectively. In silico, ADMET was used to examine their pharmacokinetic properties. ADMET (absorption, distribution, metabolism, excretion, and toxicity) studies were applied to develop new anticancer compound(s) with high selectivity. [GRAPHICS] .Publication Metadata only Synthesis and antimicrobial activity of some new 1-[4-(4-fluorobenzoylamino)-benzoyl]-4-substituted thiosemicarbazides(1995) KARAKUŞ, SEVGİ; Durgun, B. B.; Rollas, S.; Apaydin, S.; Oztürk, R.1-Aroyl-4-substituted thiosemicarbazides were obtained by the addition of 4-(4-fluorobenzoylamino)benzoylhydrazine to methyl, ethyl, propyl, allyl, cyclohexyl, phenyl and phenethyl isothiocyanates. The structures of the synthesized compounds were confirmed using UV, IR, 1H-NMR (for compounds 4c, 4g) and mass (for compounds 4b, 4c, 4g) spectral methods together with elemental analyses. None of the synthesized compounds has been reported previously.Publication Metadata only Synthesis and Anticonvulsant Activity of New N-(Alkyl/Substituted aryl)-N '-[4-(5-cyclohexylamino)-1,3,4-thiadiazole-2-yl)pheny]thioureas(WILEY-V C H VERLAG GMBH, 2009) KAYMAKÇIOĞLU, BEDİA; Karakus, Sevgi; Kocyigit-Kaymakcioglu, Bedia; Toklu, Hale Z.; Aricioglu, Feyza; Rollas, SevimA series of novel thiourea derivatives carrying the 5-cylohexylamino-1,3,4-thiadiazole moiety was synthesized and their anticonvulsant activity was evaluated. Structures of the synthesized compounds have been confirmed by IR, H-1-NMR, and elemental analysis. All of the compounds were administered at a dose of 50 mg/kg. Some of the active compounds have different effects in pentylenetetrazole (PTZ) and maximal electroshock (MES) tests, indicating the therapeutical potential in petit mal seizures, but not in grand mal seizures. Compounds 10, 11, 13, and 14 carrying 2-methylphenyl, 4-chlorophenyl, allyl, and 4-methylphenyl on the thiourea pharmacophore, increased the survival rate in the PTZ model. The ED50 values of the active compounds 10, 11, 13, and 14 were found 68.42, 43.75, 18.75 and 25 mg/kg, respectively.Publication Metadata only Synthesis and antituberculosis activity of new N-phenyl-N'-[4-(5-alkyl/arylamino-1,3,4-thiadiazole-2-yl)phenyl]thioureas(2002) KARAKUŞ, SEVGİ; Karakuş, S.; Rollas, S.In this study, eight original N-phenyl-N'-[4-(5-alkyl/arylamino-1,3,4-thiadiazole-2-yl)phenyl]thiourea derivatives were synthesized and tested for antituberculosis activity. Antituberculosis activities of the synthesized compounds were screened in vitro using BACTEC 460 Radiometric System against Mycobacterium tuberculosis H37Rv at 6.25 microg/ml. The highest inhibition observed with the synthesized compounds is 67% for N-phenyl-N'-[4-(5-cyclohexylamino-1,3,4-thiadiazole-2-yl)phenyl]thiourea.Publication Metadata only Therapeutic drug monitoring in pediatric patients treated with anti-tuberculosis medications by high performance liquid chromatography(2022-01-01) OKUYAN, BETÜL; TOK, FATİH; KARAKUŞ, SEVGİ; KAYMAKÇIOĞLU, BEDİA; SANCAR, MESUT; OKUYAN B., TOK F., KARAKUŞ S., Dalgiç N., ÇAKIR E., Midyat L., Koçyiğit-Kaymakçioğlu B., Berk U. E. , İZZETTİN F. V. , Rollas S., et al.© 2022 Marmara University Press.The aim of this study is to perform therapeutic drug monitoring for isoniazid (INH), rifampicin (RIF), and pyrazinamide (PZA) in pediatric tuberculosis patients. The study was carried out in 3 different training-research hospitals in Istanbul, Türkiye between 2011 and 2012. The pediatric patients (aged ≤14 years) who initiated the standard primary anti-tuberculosis therapy were included in this study. The serum samples were collected 3 hours after the first medication doses were given on the 5th day of treatment. Chromatographic experiments were performed on an Agilent 1100 High-Performance Liquid Chromatography (HPLC) system, and the separation was carried out on a Nova-Pak C18 (3.9x150 mm, 5 μm, Merck) analytical column. In this HPLC method, the gradient elusion delivered 3% to 40% (v/v) acetonitrile in phosphate buffer was used, and diode array detector. Twenty-three children (60.9% male) patients were included with a mean age of 111.70 ± 59.94 months. Plasma levels were measured sub-therapeutically for INH in 14, RIF in 10, and PZA in 5 patients, according to the normal range of adult patients. Maximum plasma concentrations after three hours were found between 0.53-14.02 mg/L for INH, 11.17-60.39 mg/L for PZA, 2.15-16.75 mg/L for RIF. In conclusion, this method has been successfully applied to simultaneously determine RIF, INH, and PZA plasma levels in pediatric tuberculosis patients. RIF and INH plasma levels were found to be lower in pediatric patients with tuberculosis compared to target range of adult patients.Publication Metadata only Development and validation of a rapid RP-HPLC method for the determination of cetirizine or fexofenadine with pseudoephedrine in binary pharmaceutical dosage forms(ELSEVIER SCIENCE BV, 2008) KARAKUŞ, SEVGİ; Karakus, Sevgi; Kuecuekguezel, Ilkay; Kuecuekguezel, S. GuenizThe objective of the current study was to develop a simple, accurate, precise and rapid reversed-phase HPLC method and subsequent validation using ICH suggested approach for the determination of antihistaminic-decongestant pharmaceutical dosage forms containing binary mixtures of pseudoephedrine hydrochloride (PSE) with fexofenadine hydrochloride (FEX) or cetirizine dihydrochloride (CET). The chromatographic separation of PSE, FEX and CET was achieved on a Zorbax C8 (150 mm x 4.6 mm; 5 mu m particle size) column using UV detection at 218 and 222 nm. The optimized mobile phase was consisted of TEA solution (0.5%, pH 4.5)-methanol-acetonitrile (50:20:30, v/v/v). The retention times were 1.099, 2.714 and 3.808 min for PSE, FEX and CET, respectively. The proposed method provided linear responses within the concentration ranges 30-240 and 1.25-10 mu g ml(-1) with LOD values of 1.75 and 0. 10 mu g ml(-1) for PSE and CET, respectively. Linearity range for PSE-FEX binary mixtures were 10-80 and 5-40 mu g ml(-1) with LOD values of 0.75 and 0.27 mu g ml(-1) for PSE and FEX, respectively. Correlation coefficients (r) of the regression equations were greater than 0.999 in all cases. The precision of the method was demonstrated using intra- and inter-day assay R.S.D. values which were less than 1% in all instances. No interference from any components of pharmaceutical dosage forms or degradation products was observed. According to the validation results, the proposed method was found to be specific, accurate, precise and could be applied to the quantitative analysis of these drugs in capsules containing PSE-CET or extended-release tablets containing PSE-FEX binary mixtures. (C) 2007 Elsevier B.V. All rights reserved.Publication Metadata only Synthesis of new hydrazide-hydrazone derived from etophenamate and investigation of their antimicrobial activity(2023-10-22) GÜRBÜZ, BURÇAK; RAYAMAN, PERVİN; KARAKUŞ, SEVGİ; Saral Çakmak S., GÜRBÜZ B., RAYAMAN P., KARAKUŞ S.Recently since the emerging resistant strains to antimicrobial agents, the development of original antimicrobial agents in pharmaceutical chemistry has gained great importance. Antibiotic resistance is accepted as one of the greatest threatens against health worldwide. Since 1950s to now it is known that hydrazide-hydrazones have antimicrobial, anticancer, antitubercular, anticonvulsant etc., biological spectrum and biological activity (Polovic et al., 2019). Hydrazone derivatives are used in treatment and involved in the structure of many drugs such as nifuroxazide, nitrofurazone, bisanthren, budralazine, and levosimendan. Etophenamate was chosen as the starting compound to synthesis of 16 novel hydrazide-hydrazones. All of these derivatives were investigated in order to determine their antimicrobial activities. The structures of the synthesized compounds were characterized by IR, 1H-NMR, 13C-NMR, mass spectroscopy and elemental analysis. In this study, the antimicrobial activity of 16 hydrazide-hydrazone derivatives to 4 standard bacterial strains (Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853, Enterococcus faecalis ATCC 29212) and 4 standard yeast strains (Candida albicans ATCC 90028, Candida glabrata ATCC 90030, Candida parapsilosis ATCC 90018, Candida tropicalis KUEN 1021) was examined by the microdilution method in accordance with the Clinical and Laboratory Standards Institute (CLSI) standards, and the Minimal Inhibitory Concentration (MIC) values of these derivatives were determined. It was found that among these derivatives, 2c (725-0.35µg/ml) and 2p (1000-0.5µg/ml) possed antimicrobial activity against all of the 8 standard microorganism strains.Publication Metadata only 2-Propylamino-5-[4-(2-hydroxy-3,5-dichlorobenzylideneamino) phenyl]-1,3,4-thiadiazole: X-ray and DFT-calculated structures(SPRINGER/PLENUM PUBLISHERS, 2010) KARAKUŞ, SEVGİ; Suleymanoglu, Nevin; Ustabas, Resat; Alpaslan, Yelda Bingoel; Coruh, Ufuk; Karakus, Sevgi; Rollas, Sevim2-Propylamino-5-[4-(2-hydroxy-3,5-dichlorobenzylideneamino) phenyl]-1,3,4-thiadiazole, formulated as C18H16Cl2N4OS (I), was synthesized. The crystal and molecular structure of (I) have been determined by H-1-NMR, IR, and X-ray single crystal diffraction. The compound (I) crystallizes in the monoclinic, space group P2(1)/c with unit cell parameters a = 9.0576(2) , b = 24.3382(8) , c = 9.0585(2) , M (r) = 407.31, V = 1851.13(9) (3), Z = 4, R (1) = 0.036, and wR (2) = 0.096. Molecular geometry from X-ray experiment of (I) in the ground state has been compared using the density functional method (B3LYP) with 6-31G(d) basis set. To determine conformational flexibility, molecular energy profile of (I) was obtained by semi-empirical (PM3) calculations with respect to selected degree of torsional freedom, which was varied from -180A degrees to +180A degrees in steps of 10A degrees. The results are indicative that the Schiff base, which contains a thiadiazole ring, prefers to be in E-configuration. In addition, molecular electrostatic potential, frontier molecular orbitals, and natural bond orbitals analysis were performed by the B3LYP/6-31G(d) method.