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KARAKUŞ, SEVGİ

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KARAKUŞ

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2016 - 20182
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Start date: 2010 × Subject: AGENTS ×

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    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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    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] .