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Synthesis and characterization of new 1,3,4-thiadiazole derivatives: study of their antibacterial activity and CT-DNA binding   
Yazarlar
Hakan Sezgin Sayiner
Türkiye
Mehmet Yılmazer
Türkiye
Aisha. T. Abdelsalam
Mohamed A. Ganim
Mehmet Cengiz Kayacan
Türkiye
Prof. Dr. Yasemin ÇELİK ALTUNOĞLU
Kastamonu Üniversitesi, Türkiye
Doç. Dr. Mahmut GÜR
Kastamonu Üniversitesi, Türkiye
Murat Saraçoğlu
Erciyes Üniversitesi, Türkiye
Mohamed S. Attia
Safwat A. Mahmoud
Ekram H. Mohamed
Rabah Boukherroub,
Sarah Alharthi
Nora Hamad Al- Shaalan
Prof. Dr. Fatma KANDEMİRLİ
Kastamonu Üniversitesi, Türkiye
Mohammed A. Amin
Özet
1,3,4-Thiadiazole molecules (1-4) were synthesized by the reaction of phenylthiosemicarbazide and methoxy cinnamic acid molecules in the presence of phosphorus oxychloride, and characterized with UV, FT-IR, 13C-NMR, and 1H-NMR methods. DFT calculations (b3lyp/6-311++G(d,p)) were performed to investigate the structures' geometry and physiochemical properties. Their antibacterial activity was screened for various bacteria strains such as Enterobacter aerogenes, Escherichia coli ATCC 13048, Salmonella kentucky, Pseudomonas aeruginosa, Klebsiella pneumoniae, Proteus and Gram positive such as Staphylococcus aureus ATCC 25923, Listeria monocytogenes ATCC 7644, Enterococcus faecium, Enterococcus durans, Staphylococcus aureus ATCC, Serratia marcescens, Staphylococcus hominis, Staphylococcus epidermidis, alfa Streptococcus haemolyticus, Enterococcus faecium and found to have an inhibitory effect on Klebsiella pneumoniae and Staphylococcus hominis, while molecules 1, 3 and 4 had an inhibitory effect on Staphylococcus epidermidis and alpha Streptococcus haemolyticus. The experimental results were supported by the docking study using the Kinase ThiM from Klebsiella pneumoniae. All the investigated compounds showed an inhibitory effect for the Staphylococcus epidermidis protein. In addition, the mechanism of the 1-4 molecule interaction with calf thymus-DNA (CT-DNA) was investigated by UV-vis spectroscopic methods.
Anahtar Kelimeler
Makale Türü Özgün Makale
Makale Alt Türü SSCI, AHCI, SCI, SCI-Exp dergilerinde yayımlanan tam makale
Dergi Adı RSC Advances
Dergi ISSN 2046-2069
Dergi Tarandığı Indeksler SCI-Expanded
Dergi Grubu Q2
Makale Dili İngilizce
Basım Tarihi 01-2022
Cilt No 12
Doi Numarası 10.1039/d2ra02435g
Makale Linki http://dx.doi.org/10.1039/d2ra02435g