Novel 1,3,4-Thiadiazole Derivatives as Antibiofilm, Antimicrobial, Efflux Pump Inhibiting Agents and Their ADMET Characterizations
Yazarlar (9)
Prof. Dr. Mahmut GÜR Kastamonu Üniversitesi, Türkiye
Öğr. Gör. Dr. Merve ZURNACI Kastamonu Üniversitesi, Türkiye
Eda Altınöz
Prof. Dr. Nesrin ŞENER Kastamonu Üniversitesi, Türkiye
Prof. Dr. Çiğdem Şahin İstanbul Medeniyet Üniversitesi, Türkiye
Merve Şenturan
Prof. Dr. İzzet ŞENER Kastamonu Üniversitesi, Türkiye
Prof. Dr. Muhammet Serdar ÇAVUŞ Kastamonu Üniversitesi, Türkiye
Prof. Dr. Ergin Murat ALTUNER Kastamonu Üniversitesi, Türkiye
Makale Türü Açık Erişim Özgün Makale (Ulusal alan endekslerinde (TR Dizin, ULAKBİM) yayınlanan tam makale)
Dergi Adı Hitite journal of science and engineering
Dergi ISSN 2148-4171
Dergi Tarandığı Indeksler TR DİZİN
Makale Dili Türkçe Basım Tarihi 06-2023
Kabul Tarihi 10-05-2023 Yayınlanma Tarihi 30-06-2023
Cilt / Sayı / Sayfa 10 / 2 / 99–116 DOI 10.17350/HJSE19030000297
Makale Linki http://dx.doi.org/10.17350/hjse19030000297
UAK Araştırma Alanları
Organik Kimya
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