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BİNGÖL ÖZAKPINAR, ÖZLEM

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BİNGÖL ÖZAKPINAR

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ÖZLEM

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2017 - 20202
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Author: KÜÇÜKGÜZEL, İLKAY × Subject: DRUG DISCOVERY ×

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Now showing 1 - 2 of 2
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    PublicationOpen Access
    Synthesis, characterization and biological evaluation of thioureas, acylthioureas and 4-thiazolidinones as anticancer and antiviral agents
    (MARMARA UNIV, FAC PHARMACY, 2017-04-01) ÖZSAVCI, DERYA; Kulabas, Necla; Ozakpinar, Ozlem Bingol; Ozsavci, Derya; Leyssen, Pieter; Neyts, Johan; Kucukguzel, Ilkay
    In this study, thiourea derivatives [1-4] were synthesized by using 2-amino-4-substituted pyridine compounds and these compounds have been used as the starting materials for synthesis of 2-imino-1,3-thiazolidin-4-one ring [5, 6]. Two different procedures for 4-thiazolidinone ring closure and synthesis method were optimized. The synthesized compounds were identified by the help of elemental analysis, IR, H-1-NMR, C-13-NMR and mass spectral data while the purities of them were proved with TLC. Synthesized compounds were evaluated for their antiviral and anticancer activity. Antiviral activity against Murine norovirus, Yellow fever, Enterovirus and Chikungunya strains of the test compounds were investigated and EC 50 values of these compounds were determined higher than 0,3 mu M. Cytotoxicity of test compounds was examined on NIH3T3 cell line. When the anticancer activity of test compounds was examined against PC-3, A549, HeLa, HT-29, MCF-7, SJSA1 and K562 cell lines, the percent proliferation values of these compounds were observed over 61% for all cell lines.
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    PublicationOpen Access
    Synthesis and Anticancer and Antimicrobial Evaluation of Novel Ether-linked Derivatives of Ornidazole
    (TURKISH PHARMACISTS ASSOC, 2020-02-01) KÜÇÜKGÜZEL, İLKAY; Senkardes, Sevil; Kulabas, Necta; Bingol Ozakpinar, Ozlem; Kalayci, Sadik; Sahin, Fikrettin; Kucukguzel, Ilkay; Kucukguzel, S. Guniz
    Objectives: Some novel 1-(2-methyl-5-nitro-1H-imidazol-1-yl)-3-(substituted phenoxy)propan-2-ol derivatives (3a-g) were designed and synthesized. Materials and Methods: Compounds 3a-g were obtained by refluxing ornidazole (1) with the corresponding phenolic compounds (2a-g) in the presence of anhydrous K2CO3 in acetonitrile. Results: Following the structure elucidation, the in vitro antimicrobial activity and cytotoxic effects of compounds 3a-g on K562 leukemia and NIH/3T3 mouse embryonic fibroblast cells were measured. As a part of this study, the compliance of the compounds with the drug-likeness properties was evaluated. The physico-chemical parameters (log P, TPSA, nrotb, number of hydrogen bond donors and acceptors, logS) were calculated using the software OSIRIS. Conclusion: All the synthesized compounds except 3a showed significant activity (MIC=4-16 mu g mL(-)(1)) against the bacterial strain Bacillus subtilis as compared to the standard drug, whereas antileukemic activities were rather limited. Furthermore, all the compounds were nontoxic and the selectivity index outcome indicated that the antileukemic and antimicrobial effects of the compounds were selective with good estimated oral bioavailability and drug-likeness scores.