Arylthio analogs of 5,8-quinolinedione: Synthesis, characterization, antibacterial, and antifungal evaluations
PHOSPHORUS SULFUR AND SILICON AND THE RELATED ELEMENTS, cilt.195, ss.516-522, 2020 (SCI-Expanded, Scopus)
- Yayın Türü: Makale / Tam Makale
- Cilt numarası: 195
- Basım Tarihi: 2020
- Doi Numarası: 10.1080/10426507.2020.1723097
- Dergi Adı: PHOSPHORUS SULFUR AND SILICON AND THE RELATED ELEMENTS
- Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Academic Search Premier
- Sayfa Sayıları: ss.516-522
- Anahtar Kelimeler: 67-Bis(arylthio) 58-quinolinedione, antibacterial activity, antifungal activity, CYTOTOXICITY EVALUATION, DERIVATIVES
- Açık Arşiv Koleksiyonu: AVESİS Açık Erişim Koleksiyonu
- İstanbul Üniversitesi-Cerrahpaşa Adresli: Evet
Özet
A set of bis(arylthio) substituted 5,8-quinolinedione derivatives were synthesized and investigated for their in vitro antimicrobial effect. The antibacterial and antifungal activities of 6,7-bis(arylthio)-5,8-quinolinedione (4a-f) and 6,7-bis(arylthio)-2-methyl-5,8-quinolinedione (5a-f) were evaluated against four gram-negative bacteria, three gram-positive bacteria, and three fungi strains. The bis(methoxyarylthio) 5,8-quinolinedione analogs presented better activity against especially gram-positive bacteria compared to bis(halogenarylthio) 5,8-quinolinedione analogs. Bis(3-methoxyarylthio) 5,8-quinolinedione (4e) had the same activity of the reference drug against Staphylococcus aureus. Bis(2-methoxyarylthio) 5,8-quinolinedione (4f) showed two-and-a half-fold better activity with 89.69 mu M against Enterococcus faecalis, and two-fold better activity with 11.20 mu M against Staphylococcus epidermidis. Bis(2-methoxyarylthio)-2-methyl-5,8-quinolinedione 5f exhibited five-fold higher antibacterial activity with 43.44 mu M against E. faecalis and also eight-fold activity of the reference drug with 2.71 mu M against S. epidermidis.