Thiazolidin-4-Ones as Potential Antimicrobial Agents: Experimental and In Silico Evaluation
2022
Authors:
Tratrat, ChristophePetrou, Anthi
Geronikaki, Athina
Ivanov, Marija
Kostić, Marina
Soković, Marina
Vizirianakis, Ioannis S.
Theodoroula, Nikoleta F.
Haroun, Michelyne
Document Type:
Article (Published version)
Metadata
Show full item recordAbstract:
Herein, we report computational and experimental evaluations of the antimicrobial activity of twenty one 2,3-diaryl-thiazolidin-4-ones. All synthesized compounds exhibited an antibacterial activity against six Gram-positive and Gram-negative bacteria to different extents. Thus, the MIC was in the range of 0.008–0.24 mg/mL, while the MBC was 0.0016–0.48 mg/mL. The most sensitive bacterium was S. Typhimurium, whereas S. aureus was the most resistant. The best antibacterial activity was observed for compound 5 (MIC at 0.008–0.06 mg/mL). The three most active compounds 5, 8, and 15, as well as compound 6, which were evaluated against three resistant strains, MRSA, P. aeruginosa, and E. coli, were more potent against all bacterial strains used than ampicillin. The antifungal activity of some compounds exceeded or were equipotent with those of the reference antifungal agents bifonazole and ketoconazole. The best activity was expressed by compound 5. All compounds exhibited moderate to good drug-likeness scores ranging from −0.39 to 0.39. The docking studies indicated a probable involvement of E. coli Mur B inhibition in the antibacterial action, while CYP51 inhibition is likely responsible for the antifungal activity of the tested compounds. Finally, the assessment of cellular cytotoxicity of the compounds in normal human MRC-5 cells revealed that the compounds were not toxic. View Full-Text
Keywords:
Thiazolidine-4-one; Antibacterial; Antifungal; Microdilution method; Docking; MurB; CYP51; MRC-5Source:
Molecules, 2022, 27, 6, 1930-Funding / projects:
- Ministry of Science, Technological Development and Innovation of the Republic of Serbia, institutional funding - 200007 (University of Belgrade, Institute for Biological Research 'Siniša Stanković') (RS-MESTD-inst-2020-200007)
- Deanship of Scientific Research of King Faisal University (project number 160006)
DOI: 10.3390/molecules27061930
ISSN: 1420-3049