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Novel 1,3,4-Thiadiazole Derivatives as Antibiofilm, Antimicrobial, Efflux Pump Inhibiting Agents and Their ADMET Characterizations     
Yazarlar
Doç. Dr. Mahmut GÜR
Kastamonu Üniversitesi, Türkiye
Öğr. Gör. Merve ZURNACI
Kastamonu Üniversitesi, Türkiye
Eda Altınöz
Prof. Dr. Nesrin ŞENER
Kastamonu Üniversitesi, Türkiye
Çiğdem Şahin
Türkiye
Merve Şahinturan
Prof. Dr. İzzet ŞENER
Kastamonu Üniversitesi, Türkiye
Doç. Dr. Muhammet Serdar ÇAVUŞ
Kastamonu Üniversitesi, Türkiye
Prof. Dr. Ergin Murat ALTUNER
Kastamonu Üniversitesi, Türkiye
Özet
In this study, 1,3,4-thiadiazole derivatives were obtained from the reaction of benzophenone-4,4'-dicarboxylic acid and N-substitute-thiosemicarbazide compounds with each other. After the synthesis of the final products, some biological properties of these compounds such as antibiofilm, antimicrobial and efflux pump inhibiting efficiencies were evaluated. According to the MBC/MFC test, all the activities were found to be bacteriostatic, also, especially the biofilm inhibition activity of C1 against K. pneumoniae is noteworthy. In addition, C4 was observed to exhibit efflux pump inhibition activity in E. coli, whereas C2 and C3 in K. pneumoniae. The absorption and emission values of the molecules were obtained and electrochemical studies were performed. In addition; absorption, metabolism, distribution, excretion and toxicity (ADMET) scores were predicted using the pharmacokinetic properties of all 1,3,4-thiadiazole compounds. Finally, the electrochemical stabilities of the synthesized molecules have been analyzed by using cyclic voltammetry in 0.1 M TBAPF6 in DMSO as a supporting electrolyte.
Anahtar Kelimeler
Efflux pump inhibition,antibiofilm,antibacterial,ADMET,QSAR
Makale Türü Özgün Makale
Makale Alt Türü Ulusal alan endekslerinde (TR Dizin, ULAKBİM) yayımlanan tam makale
Dergi Adı Hittite Journal of Science and Engineering
Dergi ISSN 2148-4171
Dergi Tarandığı Indeksler TR DİZİN
Makale Dili Türkçe
Basım Tarihi 06-2023
Cilt No 10
Sayı 2
Sayfalar 99 / 116
Doi Numarası 10.17350/HJSE19030000297
Makale Linki http://dx.doi.org/10.17350/hjse19030000297