TY  - JOUR
AU  - Petrou, Anthi
AU  - Geronikaki, Athina
AU  - Kartsev, Victor
AU  - Kousaxidis, Antonios
AU  - Papadimitriou-Tsantarliotou, Aliki
AU  - Kostić, Marina
AU  - Ivanov, Marija
AU  - Soković, Marina
AU  - Nicolaou, Ioannis
AU  - Vizirianakis, Ioannis S.
PY  - 2023
UR  - https://www.mdpi.com/1424-8247/16/1/131
UR  - http://www.pubmedcentral.nih.gov/articlerender.fcgi?artid=PMC9865890
UR  - http://radar.ibiss.bg.ac.rs/handle/123456789/5459
AB  - Herein, we report the experimental evaluation of the antimicrobial activity of seventeen new (Z)-methyl 3-(4-oxo-2-thioxothiazolidin-5-ylidene)methyl)-1H-indole-2-carboxylate derivatives. All tested compounds exhibited antibacterial activity against eight Gram-positive and Gram-negative bacteria. Their activity exceeded those of ampicillin as well as streptomycin by 10-50 fold. The most sensitive bacterium was En. Cloacae, while E. coli was the most resistant one, followed by M. flavus. The most active compound appeared to be compound 8 with MIC at 0.004-0.03 mg/mL and MBC at 0.008-0.06 mg/mL. The antifungal activity of tested compounds was good to excellent with MIC in the range of 0.004-0.06 mg/mL, with compound 15 being the most potent. T. viride was the most sensitive fungal, while A. fumigatus was the most resistant one. Docking studies revealed that the inhibition of E. coli MurB is probably responsible for their antibacterial activity, while 14a-lanosterol demethylase of CYP51Ca is involved in the mechanism of antifungal activity. Furthermore, drug-likeness and ADMET profile prediction were performed. Finally, the cytotoxicity studies were performed for the most active compounds using MTT assay against normal MRC5 cells.
PB  - Basel: MDPI
T2  - Pharmaceuticals
T1  - N-Derivatives of (Z)-Methyl 3-(4-Oxo-2-thioxothiazolidin-5-ylidene)methyl)-1H-indole-2-carboxylates as Antimicrobial Agents-In Silico and In Vitro Evaluation
IS  - 1
VL  - 16
DO  - 10.3390/ph16010131
SP  - 131
ER  - 

@article{
author = "Petrou, Anthi and Geronikaki, Athina and Kartsev, Victor and Kousaxidis, Antonios and Papadimitriou-Tsantarliotou, Aliki and Kostić, Marina and Ivanov, Marija and Soković, Marina and Nicolaou, Ioannis and Vizirianakis, Ioannis S.",
year = "2023",
abstract = "Herein, we report the experimental evaluation of the antimicrobial activity of seventeen new (Z)-methyl 3-(4-oxo-2-thioxothiazolidin-5-ylidene)methyl)-1H-indole-2-carboxylate derivatives. All tested compounds exhibited antibacterial activity against eight Gram-positive and Gram-negative bacteria. Their activity exceeded those of ampicillin as well as streptomycin by 10-50 fold. The most sensitive bacterium was En. Cloacae, while E. coli was the most resistant one, followed by M. flavus. The most active compound appeared to be compound 8 with MIC at 0.004-0.03 mg/mL and MBC at 0.008-0.06 mg/mL. The antifungal activity of tested compounds was good to excellent with MIC in the range of 0.004-0.06 mg/mL, with compound 15 being the most potent. T. viride was the most sensitive fungal, while A. fumigatus was the most resistant one. Docking studies revealed that the inhibition of E. coli MurB is probably responsible for their antibacterial activity, while 14a-lanosterol demethylase of CYP51Ca is involved in the mechanism of antifungal activity. Furthermore, drug-likeness and ADMET profile prediction were performed. Finally, the cytotoxicity studies were performed for the most active compounds using MTT assay against normal MRC5 cells.",
publisher = "Basel: MDPI",
journal = "Pharmaceuticals",
title = "N-Derivatives of (Z)-Methyl 3-(4-Oxo-2-thioxothiazolidin-5-ylidene)methyl)-1H-indole-2-carboxylates as Antimicrobial Agents-In Silico and In Vitro Evaluation",
number = "1",
volume = "16",
doi = "10.3390/ph16010131",
pages = "131"
}

Petrou, A., Geronikaki, A., Kartsev, V., Kousaxidis, A., Papadimitriou-Tsantarliotou, A., Kostić, M., Ivanov, M., Soković, M., Nicolaou, I.,& Vizirianakis, I. S.. (2023). N-Derivatives of (Z)-Methyl 3-(4-Oxo-2-thioxothiazolidin-5-ylidene)methyl)-1H-indole-2-carboxylates as Antimicrobial Agents-In Silico and In Vitro Evaluation. in Pharmaceuticals
Basel: MDPI., 16(1), 131.
https://doi.org/10.3390/ph16010131

Petrou A, Geronikaki A, Kartsev V, Kousaxidis A, Papadimitriou-Tsantarliotou A, Kostić M, Ivanov M, Soković M, Nicolaou I, Vizirianakis IS. N-Derivatives of (Z)-Methyl 3-(4-Oxo-2-thioxothiazolidin-5-ylidene)methyl)-1H-indole-2-carboxylates as Antimicrobial Agents-In Silico and In Vitro Evaluation. in Pharmaceuticals. 2023;16(1):131.
doi:10.3390/ph16010131 .

Petrou, Anthi, Geronikaki, Athina, Kartsev, Victor, Kousaxidis, Antonios, Papadimitriou-Tsantarliotou, Aliki, Kostić, Marina, Ivanov, Marija, Soković, Marina, Nicolaou, Ioannis, Vizirianakis, Ioannis S., "N-Derivatives of (Z)-Methyl 3-(4-Oxo-2-thioxothiazolidin-5-ylidene)methyl)-1H-indole-2-carboxylates as Antimicrobial Agents-In Silico and In Vitro Evaluation" in Pharmaceuticals, 16, no. 1 (2023):131,
https://doi.org/10.3390/ph16010131 . .

TY  - JOUR
AU  - Tratrat, Christophe
AU  - Petrou, Anthi
AU  - Geronikaki, Athina
AU  - Ivanov, Marija
AU  - Kostić, Marina
AU  - Soković, Marina
AU  - Vizirianakis, Ioannis S.
AU  - Theodoroula, Nikoleta F.
AU  - Haroun, Michelyne
PY  - 2022
UR  - http://radar.ibiss.bg.ac.rs/handle/123456789/4936
AB  - 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
PB  - Basel: MDPI
T2  - Molecules
T1  - Thiazolidin-4-Ones as Potential Antimicrobial Agents: Experimental and In Silico Evaluation
IS  - 6
VL  - 27
DO  - 10.3390/molecules27061930
SP  - 1930
ER  - 

@article{
author = "Tratrat, Christophe and Petrou, Anthi and Geronikaki, Athina and Ivanov, Marija and Kostić, Marina and Soković, Marina and Vizirianakis, Ioannis S. and Theodoroula, Nikoleta F. and Haroun, Michelyne",
year = "2022",
abstract = "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",
publisher = "Basel: MDPI",
journal = "Molecules",
title = "Thiazolidin-4-Ones as Potential Antimicrobial Agents: Experimental and In Silico Evaluation",
number = "6",
volume = "27",
doi = "10.3390/molecules27061930",
pages = "1930"
}

Tratrat, C., Petrou, A., Geronikaki, A., Ivanov, M., Kostić, M., Soković, M., Vizirianakis, I. S., Theodoroula, N. F.,& Haroun, M.. (2022). Thiazolidin-4-Ones as Potential Antimicrobial Agents: Experimental and In Silico Evaluation. in Molecules
Basel: MDPI., 27(6), 1930.
https://doi.org/10.3390/molecules27061930

Tratrat C, Petrou A, Geronikaki A, Ivanov M, Kostić M, Soković M, Vizirianakis IS, Theodoroula NF, Haroun M. Thiazolidin-4-Ones as Potential Antimicrobial Agents: Experimental and In Silico Evaluation. in Molecules. 2022;27(6):1930.
doi:10.3390/molecules27061930 .

Tratrat, Christophe, Petrou, Anthi, Geronikaki, Athina, Ivanov, Marija, Kostić, Marina, Soković, Marina, Vizirianakis, Ioannis S., Theodoroula, Nikoleta F., Haroun, Michelyne, "Thiazolidin-4-Ones as Potential Antimicrobial Agents: Experimental and In Silico Evaluation" in Molecules, 27, no. 6 (2022):1930,
https://doi.org/10.3390/molecules27061930 . .