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  • Küçük Resim Yok
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    AZI 4,5-DİHİDRO-1H-PİRAZOL VE ŞALKON TÜREVLERİNİN ANTİMİKROBİYAL VE ANTİTÜBERKÜLER ETKİLERİ ÜZERİNE ARAŞTIRMALAR
    (2021) Evranos-Aksöz, Begüm; Onurdağ, Fatma Kaynak; Aksöz, Erkan; Özgacar, Selda Özgen
    Amaç: Bu çalışmada öncelikle şalkonlar ve bu şalkon türevlerinin hidrazitler ile reaksiyonu sonucu halka kapanması ile oluşan 4,5-dihidro-1H-pirazol yapısındaki bileşikler sentez edilmiş ve sentezlenen tüm bileşiklerin antimikrobiyal ve antitüberküler etkileri araştırılmıştır. Gereç ve Yöntem: Benzaldehit ve asetofenon türevlerinin alkali ortamda metanol içindeki reaksiyonuyla elde edilen şalkonların, hidrazit türevleri ile etanol içindeki reaksiyonu sonucu 4,5-dihidro-1H-pirazol türevleri elde edilmiştir. Sentezlenen bu bileşiklerin antimikrobiyal etkileri mikrodilüsyon yöntemiyle, antitüberküler etkileri ise mikroplaka alamar mavisi deneyi ile saptanmıştır. Sonuç ve Tartışma: Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853, Pseudomonas aeruginosa izolat (gentamisine dirençli) ve Candida albicans’a karşı 4,5-dihidro-1H-pirazol yapısındaki bileşiklerin şalkonlardan daha etkili olduğu bulunmuştur. Staphylococcus aureus’a karşı ise şalkonlar 4,5-dihidro-1H-pirazol türevlerinden daha etkili bulunmuştur. Staphylococcus aureus izolat (MRSA) ve Mycobacterium tuberculosis’e karşı hem şalkonlar hem de 4,5-dihidro-1H-pirazol türevleri aynı etkiyi göstermiştir. B21 bileşiği Candida krusei üzerinde flukonazolle aynı etkiyi göstermiştir. B20 bileşiği ise Candida krusei üzerine flukonazolden daha etkili bulunmuştur. Anahtar kelimeler: Antimikrobiyal etki, antitüberküler etki, 4,5-dihidro-1H-pirazol, şalkon
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    In Silico ADME Screening and Evaluation of Antimicrobial and Antimycobacterial Activities of 3,5-Diphenyl Pyrazoline Derivatives
    (2021) Evranos-Aksöz, Begüm; Onurdağ, Fatma Kaynak; Aksöz, Erkan; Özgacar, Selda Özgen
    Objective: The unconscious widespread use of antibiotics leads to the development of resistance to antibiotics. When resistance to an antibiotic develops, it now either shows less efficacy or loses its effect completely at that antibiotic treatment dose. While the development of resistance to antibiotics increases rapidly, the need for the development of new antibiotics rises every day. For this purpose, in this study, antimicrobial and antitubercular effects of some compounds in the pyrazoline structure were investigated. The physicochemical properties and drug-likeness of the compounds are quite important for determining whether a compound can be used as a drug or not. Physicochemical properties and drug-likeness of the synthesized compounds were evaluated and the relevance for Lipinski’s rules was determined. Material- Method: Drug-likeness properties of the synthesized compounds were determined using online Swiss ADME tool. Antitubercular activity is detected by microplate alamar blue assay. Antimicrobial activity is tested by microdilution method. Results: All compounds obeyed the Lipinski’s rules, some of with no violation, some of with one violation. Compounds B7, B10 and B11 provided Lipinski’s rules with one violation. Other compounds ensured Lipinski’s rules with no violation. All compounds were predicted to have high gastrointestinal absorption. As the compounds generally have high lipophilicity, it was predicted that all compounds except B12 can cross the blood brain barrier. Conclusion: Synthesized compounds were mostly found to be more effective against Enterococcus faecalis, Enterococcus faecalis isolate and Candida albicans. Compound B10 demonstrated the best antimicrobial activity against Enterococcus faecalis isolate with a 16?g/mL MIC value.
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    Investigation of Antimicrobial and Antitubercular Activities of Some Hydrazone DerivedCompounds
    (2020) Evranos-Aksöz, Begüm; Onurdağ, Fatma Kaynak; Aksöz, Erkan; Özgacar, Selda Özgen
    Aseriesofhydrazonederivativesweresynthesizedtoinvestigate antifungal,antimicrobialandantitubercularactivities.Theseactivitieswere investigatedagainst Escherichiacoli, Escherichiacoli isolate, Pseudomonas aeruginosa, Pseudomonas aeruginosaisolate (resistant to gentamicin), Staphylococcus aureus, Staphylococcus aureus isolate (MRSA), Enterococcusfaecalis, Enterococcusfaecalis isolate(VRE), Candidaalbicans, Candidakrusei andMycobacteriumtuberculosis. Among the synthesized compounds B23had the best activity against Candida albicanswith 16 ?g/mL MIC value and B24had the best activity against Staphylococcus aureus isolate (MRSA) with 16 ?g/mL MIC value. The most effective compound against Mycobacteriumtuberculosis is found to be E9 with 32 ?g/mL MIC value, achalcone derivative. However, all compounds were determined as ineffective against Escherichia coli and Escherichia coli isolate.