Trifloroasetofenon oksim ester türevlerinin sentezi ve biyolojik aktiviteleri üzerindeki çalışmalar
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Dosyalar
Tarih
2018
Yazarlar
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Yayıncı
İnönü Üniversitesi
Erişim Hakkı
info:eu-repo/semantics/openAccess
Özet
Amaç: Enfeksiyon hastalıkları, dünya genelinde ciddi bir sağlık sorunudur ve insan morbiditesi ve mortalitesinin ana nedenlerinden biridir. Mevcut ilaçların dar aktivite spektrumu, toksisitesi, zayıf farmakokinetik özellikleri ve ilaçlara karşı direnç gelişmesinden dolayı etkili antifungal ve antibakteriyel bileşikler geliştirmek için yoğun çalışmalar yapılmaktadır. Bu çalışmada azol grubu antifungal ilaçların yapısı esas alınarak tasarlanan bir seri yeni bileşik, 1-(4-triflorometilfenil)-2-(1H-imidazol-1-il)etanon oksim esterlerin antifungal, antibakteriyel ve sitotoksik etkilerinin incelenmesi amaçlanmıştır. Materyal ve Metot: Bu çalışmada 21 yeni bileşiğin sentezi yapılmış ve bileşiklerin yapıları spektral analiz verileriyle aydınlatılmıştır. Sentezlenen bileşiklerin antifungal aktiviteleri üç Candida türüne, antibakteriyel aktiviteleri de dört bakteri türüne karşı incelenmiştir. In vitro sitotoksisite aktiviteleri ise L929 ve SH-SY5Y hücre hatlarına karşı incelenmiştir. Bulgular: Yapılan çalışmalar sonucunda bileşikler Candida türlerine karşı orta derecede etkiliyken, bakteri türlerine karşı daha etkili bulunmuştur. Bazı bileşikler S.aureus'a karşı MIK değeri 4 µg/ml bulunmuştur. Bileşiklerin hücre hatlarına karşı % hücre canlılık ve IC50 değerleri hesaplanmıştır. Bileşikler L929 hücre hattına önemli sitotoksik etkiler göstermezken, SH-SYSH hücre hattına karşı etkili bulunmuştur. Sonuç: 21 yeni bileşiğin sentezi yapılıp, antifungal, antibakteriyel ve sitotoksik etkileri incelenmiştir. Elde edilen sonuçlara göre antifungal aktivitesi yüksek ve SH-SY5Y hücre hattında daha etkili olabilecek bileşikler tasarlanacaktır. Anahtar Kelimeler: Antibakteriyel, antifungal, imidazol, oksim, sitotoksisite
Aim: Infection diseases are a serious health problem worldwide and one of the main causes of human morbidity and mortality. Existing drugs have been extensively studied to develop effective antifungal and antibacterial compounds because of their narrow spectrum of activity, toxicity, poor pharmacokinetic properties and resistance to drugs. In this thesis, it was aimed to investigate the antifungal, antibacterial and cytotoxic effects of 1-(4-trifluoromethylphenyl)-2-(1H-imidazol-1-yl)ethanone oxime esters, a series of new compounds designed based on the structure of azole group antifungal drugs. Material ve Method: In this study, 21 new compounds were synthesized and the structures of the compounds were confirmed by spectral analysis. The antifungal and antibacterial activities of the synthesized compounds were examined against three Candida species and four bacterial strains. In vitro cytotoxicity activities of the compounds were investigated against L929 and SH-SY5Y cell lines. Results: As a result of the studies performed, the compounds were found to be more effective against bacterial strains, while they were moderately effective against Candida species. Some compounds were found to have a MIC value of 4 μg/ml against S.aureus. The % cell viability and IC50 values against the cell lines of the compounds were calculated. While compounds L929 did not show significant cytotoxic effects on the cell line, they was found to be effective against SH-SYSH cell line. Conclusion: 21 compounds were synthesized and their activities were investigated. According to the results obtained, compounds which have high antifungal activity and can be more effective in the SH-SY5Y cell line will be designed. Key Words: Antibacterial, antifungal, cytotoxicity, imidazole, oxime
Aim: Infection diseases are a serious health problem worldwide and one of the main causes of human morbidity and mortality. Existing drugs have been extensively studied to develop effective antifungal and antibacterial compounds because of their narrow spectrum of activity, toxicity, poor pharmacokinetic properties and resistance to drugs. In this thesis, it was aimed to investigate the antifungal, antibacterial and cytotoxic effects of 1-(4-trifluoromethylphenyl)-2-(1H-imidazol-1-yl)ethanone oxime esters, a series of new compounds designed based on the structure of azole group antifungal drugs. Material ve Method: In this study, 21 new compounds were synthesized and the structures of the compounds were confirmed by spectral analysis. The antifungal and antibacterial activities of the synthesized compounds were examined against three Candida species and four bacterial strains. In vitro cytotoxicity activities of the compounds were investigated against L929 and SH-SY5Y cell lines. Results: As a result of the studies performed, the compounds were found to be more effective against bacterial strains, while they were moderately effective against Candida species. Some compounds were found to have a MIC value of 4 μg/ml against S.aureus. The % cell viability and IC50 values against the cell lines of the compounds were calculated. While compounds L929 did not show significant cytotoxic effects on the cell line, they was found to be effective against SH-SYSH cell line. Conclusion: 21 compounds were synthesized and their activities were investigated. According to the results obtained, compounds which have high antifungal activity and can be more effective in the SH-SY5Y cell line will be designed. Key Words: Antibacterial, antifungal, cytotoxicity, imidazole, oxime
Açıklama
Anahtar Kelimeler
Eczacılık ve Farmakoloji, Pharmacy and Pharmacology
Kaynak
WoS Q Değeri
Scopus Q Değeri
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Künye
Bozbey, İ. Trifloroasetofenon oksim ester türevlerinin sentezi ve biyolojik aktiviteleri üzerindeki çalışmalar. İnönü Üniversitesi / Sağlık Bilimleri Enstitüsü / Farmasötik Kimya Anabilim Dalı. 150 s. 2018.
