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 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 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.