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KARAKUŞ, SEVGİ

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KARAKUŞ

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SEVGİ

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2010 - 20207
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Now showing 1 - 7 of 7
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    PublicationOpen Access
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    PublicationOpen Access
    Synthesis and antimycobacterial activity of some 2-(4-aminophenyl)-5-substituted amino-1,3,4-thiadiazole derivatives and their coupling products
    (MARMARA UNIV, FAC PHARMACY, 2016-02-02) KARAKUŞ, SEVGİ; Karakus, Sevgi; Rollas, Sevim
    In the present study, several 2-(4-aminophenyl)-5-substituted amino-1,3,4-thiadiazoles (2a-l) and their coupling products, 2,3,4-pentanetrione-3-[4-(5-alkyl/arylamino-1,3,4-thiadiazole-2-yl)phenyl]hydrazones (3a-j) were synthesized in good yields and characterized by UV, IR, H-1-NMR, mass and elemental analysis. Antitubercular activity of the synthesized compounds was determined in vitro using the BACTEC 460 Radiometric System against Mycobacterium tuberculosis H37Rv at 6.25 mu g/mL. The antimycobacterial data of screened compounds indicated that 2-(4-aminophenyl)-5-(4-chlorophenyl)amino-1,3,4-thiadiazole 2f demonstrated the highest inhibition.
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    PublicationOpen Access
    The synthesis and biological activities of 3-acyl- 2,3-dihydro-1,3,4-oxadiazole / 3-acyl-1,3,4-oxadiazoline derivatives obtained from hydrazide-hydrazones [Hidrazid-hidrazonlardan elde edilen 3-açil- 2,3-dihidro-1,3,4-oksadiazol / 3-açil-1,3,4-oksadiazolin türevlerinin sentezi ve biyolojik aktiviteleri]
    (2012-01-01) KARAKUŞ, SEVGİ; Rollas S., Karakuş S.
    In this review, the synthesis and biological activities of 3-acyl-2,3-dihydro-1,3,4- oxadiazole derivatives are reported. Synthesis of 1,3,4-oxadiazolines via carboxylic acid hydrazide-hydrazones by using acetic anhydride or other cyclization agents establishes the peculiar basis of our work.
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    PublicationOpen Access
    Design, Synthesis, and Molecular Docking Studies of a Conjugated-Thiadiazole Thiourea Scaffold as Antituberculosis Agents
    (PHARMACEUTICAL SOC JAPAN, 2016) TATAR, ESRA; Tatar, Esra; Karakus, Sevgi; Kucukguzel, Sukriye Guniz; Okullu, Sinem Oktem; Unubol, Nihan; Kocagoz, Tanil; De Clercq, Erik; Andrei, Graciela; Snoeck, Robert; Pannecouque, Christophe; Kalayci, Sadik; Sahin, Fikrettin; Sriram, Dharmarajan; Yogeeswari, Perumal; Kucukguzel, Ilkay
    In view of the emergence and frequency of multidrug-resistant and extensively drug-resistant tuberculosis and consequences of acquired resistance to clinically used drugs, we undertook the design and synthesis of novel prototypes that possess the advantage of the two pharmacophores of thiourea and 1,3,4-thiadiazole in a single molecular backbone. Three compounds from our series were distinguished from the others by their promising activity profiles against Mycobacterium tuberculosis strain H(37)Rv. Compounds 11 and 19 were the most active representatives with minimum inhibitory concentration (MIC) values of 10.96 and 11.48 mu m, respectively. Compound 15 was shown to inhibit M. tuberculosis strain H(37)Rv with an MIC value of 17.81 mu m. Cytotoxicity results in the Vero cell line showed that these three derivatives had selectivity indices between 1.8 and 8.7. In order to rationalize the biological results of our compounds, molecular docking studies with the enoyl acyl carrier protein reductase (InhA) of M. tuberculosis were performed and compounds 11, 15, and 19 were found to have good docking scores in the range of -7.12 to -7.83 kcal/mol.
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    PublicationOpen Access
    Synthesis, characterization, antituberculosis activity and computational studies on novel Schiff bases of 1,3,4-thiadiazole derivatives
    (MARMARA UNIV, 2020-10-15) KARAKUŞ, SEVGİ; Turk, Sevda; Karakus, Sevgi; Maryam, Arooma; Oruc-Emre, Emine Elcin
    A series of novel Schiff bases were designed and synthesized by the condensation of 1,3,4-thiadiazoles that contain aromatic primary amine and variously substituted benzaldehydes. The synthesized compounds were screened for their antituberculosis activity against Mycobacterium tuberculosis H(37)Rv using BACI EC 460 radiometric system. Among the tested compounds, 2-(4-nitrophenyl)amino-5-[4-(3-(4-phenoxy))benzylideneaminophenyl]-1,3,4-thiadiazole (3n) showed the highest inhibitory activity (80%). The activities of the newly synthesized Schiff bases were higher in comparison to those of intermediate products 2-(4-aminophenyl)-5-aryl/alkylamino-1,3,4-thiadiazoles (2a-l). The computational studies were also performed to estimate drug-like profile of the compounds by using QikProp analysis.
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    PublicationOpen Access
    The synthesis and evaluation of anti-acetylcholinesterase activity of some 4(3H)-quinazolinone derivatives bearing substituted 1,3,4- thiadiazole
    (MARMARA UNIV, FAC MEDICINE, 2016-09-09) KARAKUŞ, SEVGİ; Uraz, Mine; Karakus, Sevgi; Abu Mohsen, Usama; Kaplancikli, Zafer Asim; Rollas, Sevim
    In the present study, a series of 4(3H)-quinazolinone derivatives (5a-f) were synthesized through the cylization reaction of substituted 1,3,4-thiadiazoles containing an aromatic primary amin and anthranilic acid in the presence of acetic anhydride and acetic acid. The structures of the synthesized compounds were confirmed by elemental analysis, IR, H-1-NMR and mass spectroscopic (5b and 5f) methods. Each derivative was evaluated for its ability to inhibit acetylcholinesterase (AChE) using a modification of Ellman's spectrophotometric method. Compounds 2-methyl-3-{4-[5-(ethylamino)-1,3,4-thiadiazol-2-yl]phenyl} quinazolin-4(3H)-one (5b) and 2-methyl-3-{4-[5(cyclohexylamino)-1,3,4-thiadiazol-2-yl]phenyl} quinazolin4(3H)-one (5d) can be identified as promising anticholinesterase agents due to their inhibitory effect when compared with donepezil as a reference drug.
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    PublicationOpen Access
    Some N-(5-methyl-1,3,4-thiadiazol-2-yl)-4-[(3-substituted)ureido/thioureido]benzenesulfonamides as carbonic anhydrase I and II Inhibitors
    (MARMARA UNIV, FAC PHARMACY, 2016-08-25) KAYMAKÇIOĞLU, BEDİA; Turk, Sevda; Tok, Fatih; Celik, Hulya; Karakus, Sevgi; Nadaroglu, Hayrunnisa; Kocyigit-Kaymakcioglu, Bedia; Kucukoglu, Kaan
    In the present study, N-(5-methyl-1,3,4-thiadiazol-2-yl)-4-[(3-substituted)ureido]benzenesulfonamide (1-9) and N-(5-methyl-1,3,4-thiadiazol-2-yl)-4-[(3-substituted) thioureido]benzenesulfonamide (10-14) derivatives were synthesized from 4-amino-N-(5-methyl-1,3,4-thiadiazol-2-yl) benzenesulfonamide (sulfamethizole). All new compounds were characterized by elemental analysis and various spectroscopic methods (FTIR, H-1-NMR and MS). These new sulfonamide derivatives were investigated as inhibitors of carbonic anhydrase especially human carbonic anhydrase I and II. The new compounds showed higher activity against the human cytosolic CA I (IC50 values 0.144-15.65 nM) and CA II (IC50 values 0.109-17.95 nM) in comparison with the clinically used CA inhibitor acetazolamide.