Studies on Antimicrobial, Antibiofilm, Efflux Pump Inhibiting, and ADMET Properties of Newly Synthesized 1,3,4-Thiadiazole Derivatives

Merve Zurnaci1, Merve Senturan2, Nesrin Sener3, Mahmut Gur4*, Eda Altinoz2, Izzet Sener5, Ergin Murat Altuner6

1Kastamonu University, Central Research Laboratory, TR 37150 Kastamonu, Turkey
2Kastamonu University, Institue of Science, TR 37150 Kastamonu, Turkey
3Kastamonu University, Faculty of Science and Arts, Department of Chemistry, TR 37150 Kastamonu, Turkey
4Kastamonu University, Faculty of Forestry, Department of Forest Industrial Engineering, TR 37150 Kastamonu, Turkey
5Kastamonu University, Faculty of Engineering and Architecture, Department of Food Engineering, TR 37150 Kastamonu, Turkey
6Kastamonu University, Faculty of Science and Arts, Department of Biology, TR 37150 Kastamonu, Turkey

* Corresponding author: mahmutgur@kastamonu.edu.tr

The novel compounds bearing 1,3,4-thiadiazole moiety were obtained and their structures were identified using FT-IR, NMR methods, elemental, and mass analysis. UV-Vis and fluorescence spectra were obtained in six different polarity solvents. In addition, antimicrobial, antibiofilm, and the efflux pump inhibiting activities of the new compounds on K. pneumoniae, methicillin-resistant S. aureus (MRSA), E. coli, and C. albicans were investigated. Furthermore, druglikeness and ADMET properties of the compounds were determined. As a result, it was observed that some of the derivatives presented antimicrobial activity against K. pneumoniae, S. aureus, and C. albicans. But the MBC/MFC test showed that all the activities were bacteriostatic. In addition, these derivatives have the potential of using both inhibiting and activating biofilm formation depending on the concentration. 1,3,4-thiadiazole derivatives also presented good efflux pump inhibition in K. pneumoniae and E. coli. ADMET tests showed that 1,3,4-thiadiazole derivatives have the potential of being used as therapeutic compounds.
Keywords: 1,3,4-thiadiazole, ADMET, antibacterial, antibiofilm, efflux pump inhibition, QSAR

How to cite: Zurnaci, M., Senturan, M., Sener, N., Gür, M., Altinoz, E., Sener, I., & Altuner, E. M. (2021). Studies on Antimicrobial, Antibiofilm, Efflux Pump Inhibiting, and ADMET Properties of Newly Synthesized 1, 3, 4‐Thiadiazole Derivatives.ChemistrySelect, 6(45), 12571-12581.

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