TY  - JOUR
AU  - Haroun, Michelyne
AU  - Tratrat, Christophe
AU  - Kositsi, Katerina
AU  - Tsolaki, Evangelia
AU  - Petrou, Anthi
AU  - Aldhubiab, Bandar
AU  - Attimarad, Mahesh
AU  - Harsha, Sree
AU  - Geronikaki, Athina
AU  - Venugopala, Katharigatta N.
AU  - Elsewedy, Heba S.
AU  - Soković, Marina
AU  - Glamočlija, Jasmina
AU  - Ćirić, Ana
PY  - 2018
UR  - http://www.eurekaselect.com/159582/article
UR  - https://radar.ibiss.bg.ac.rs/handle/123456789/3071
AB  - BACKGROUND Thiazole and benzothiazole derivatives, as well as thiazolidinones are very important scaffolds in medicinal chemistry. Literature has revealed that they possess a wide spectrum of biological activities including antimicrobial activity. OBJECTIVE The goal of this paper is the designing of new benzothiazole based thiazolidinones and the evaluation of their biological activities. METHODS The designed compounds were synthesized using classical organic synthesis methods. The antimicrobial activity was evaluated using the method of microdilution. RESULTS The twelve newly synthesized compounds showed antimicrobial properties. All compounds appeared to be more active than ampicillin in most studied strains and in some cases, more active than streptomycin. Antifungal activity, in most cases was also better than the reference drugs ketoconazole and bifonazole. The prediction of cytotoxicity revealed that the synthesized compounds were not toxic (LD50 350-1000 mg/kg of body weight). Docking studies on the antibacterial activity confirmed the biological results. CONCLUSION The twelve new compounds were synthesized and studied for their antimicrobial activity. The compounds appeared to be promising antimicrobial agents and could be the lead compounds for new, more potent drugs. According to the docking prediction, the compounds could be MurB inhibitors.
T2  - Current Topics in Medicinal Chemistry
T1  - New Benzothiazole-based Thiazolidinones as Potent Antimicrobial Agents. Design, synthesis and Biological Evaluation.
IS  - 1
VL  - 18
DO  - 10.2174/1568026618666180206101814
SP  - 75
EP  - 87
ER  - 

@article{
author = "Haroun, Michelyne and Tratrat, Christophe and Kositsi, Katerina and Tsolaki, Evangelia and Petrou, Anthi and Aldhubiab, Bandar and Attimarad, Mahesh and Harsha, Sree and Geronikaki, Athina and Venugopala, Katharigatta N. and Elsewedy, Heba S. and Soković, Marina and Glamočlija, Jasmina and Ćirić, Ana",
year = "2018",
abstract = "BACKGROUND Thiazole and benzothiazole derivatives, as well as thiazolidinones are very important scaffolds in medicinal chemistry. Literature has revealed that they possess a wide spectrum of biological activities including antimicrobial activity. OBJECTIVE The goal of this paper is the designing of new benzothiazole based thiazolidinones and the evaluation of their biological activities. METHODS The designed compounds were synthesized using classical organic synthesis methods. The antimicrobial activity was evaluated using the method of microdilution. RESULTS The twelve newly synthesized compounds showed antimicrobial properties. All compounds appeared to be more active than ampicillin in most studied strains and in some cases, more active than streptomycin. Antifungal activity, in most cases was also better than the reference drugs ketoconazole and bifonazole. The prediction of cytotoxicity revealed that the synthesized compounds were not toxic (LD50 350-1000 mg/kg of body weight). Docking studies on the antibacterial activity confirmed the biological results. CONCLUSION The twelve new compounds were synthesized and studied for their antimicrobial activity. The compounds appeared to be promising antimicrobial agents and could be the lead compounds for new, more potent drugs. According to the docking prediction, the compounds could be MurB inhibitors.",
journal = "Current Topics in Medicinal Chemistry",
title = "New Benzothiazole-based Thiazolidinones as Potent Antimicrobial Agents. Design, synthesis and Biological Evaluation.",
number = "1",
volume = "18",
doi = "10.2174/1568026618666180206101814",
pages = "75-87"
}

Haroun, M., Tratrat, C., Kositsi, K., Tsolaki, E., Petrou, A., Aldhubiab, B., Attimarad, M., Harsha, S., Geronikaki, A., Venugopala, K. N., Elsewedy, H. S., Soković, M., Glamočlija, J.,& Ćirić, A.. (2018). New Benzothiazole-based Thiazolidinones as Potent Antimicrobial Agents. Design, synthesis and Biological Evaluation.. in Current Topics in Medicinal Chemistry, 18(1), 75-87.
https://doi.org/10.2174/1568026618666180206101814

Haroun M, Tratrat C, Kositsi K, Tsolaki E, Petrou A, Aldhubiab B, Attimarad M, Harsha S, Geronikaki A, Venugopala KN, Elsewedy HS, Soković M, Glamočlija J, Ćirić A. New Benzothiazole-based Thiazolidinones as Potent Antimicrobial Agents. Design, synthesis and Biological Evaluation.. in Current Topics in Medicinal Chemistry. 2018;18(1):75-87.
doi:10.2174/1568026618666180206101814 .

Haroun, Michelyne, Tratrat, Christophe, Kositsi, Katerina, Tsolaki, Evangelia, Petrou, Anthi, Aldhubiab, Bandar, Attimarad, Mahesh, Harsha, Sree, Geronikaki, Athina, Venugopala, Katharigatta N., Elsewedy, Heba S., Soković, Marina, Glamočlija, Jasmina, Ćirić, Ana, "New Benzothiazole-based Thiazolidinones as Potent Antimicrobial Agents. Design, synthesis and Biological Evaluation." in Current Topics in Medicinal Chemistry, 18, no. 1 (2018):75-87,
https://doi.org/10.2174/1568026618666180206101814 . .