Novel 1,3,4-Thiadiazole Derivatives as Antibiofilm, Antimicrobial, Efflux Pump Inhibiting Agents and Their ADMET Characterizations

Autor: Ergin Murat Altuner, Muhammet Çavuş, İzzet Şener, Merve Şenturan, Çiğdem Şahin, Nesrin Şener, Eda Altınöz, Merve Zurnacı, Mahmut Gür
Jazyk: angličtina
Rok vydání: 2023
Předmět:
Zdroj: Hittite Journal of Science and Engineering, Vol 10, Iss 2, Pp 99-116 (2023)
Druh dokumentu: article
ISSN: 2148-4171
DOI: 10.17350/HJSE19030000297
Popis: 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.
Databáze: Directory of Open Access Journals