New Benzothiazole-based Thiazolidinones as Potent Antimicrobial Agents. Design, synthesis and Biological Evaluation

Title:New Benzothiazole-based Thiazolidinones as Potent Antimicrobial Agents. Design, synthesis and Biological Evaluation

Volume: 18 Issue: 1

Author(s): Michelyne Haroun*, Christophe Tratrat, Katerina Kositzi, Evangelia Tsolaki, Anthi Petrou, Bandar Aldhubiab, Mahesh Attimarad, Sree Harsha, Athina Geronikaki*, Katharigatta N. Venugopala, Heba S. Elsewedy, Marina Sokovic, Jasna Glamoclija and Ana Ciric

Affiliation:

• Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982,Saudi Arabia

• Aristotle University, School of Pharmacy, Thessaloniki, 54124,Greece

Keywords: Benzothiazole, Thiazolidinone, Antibacterial, Antifungal, Microdilution, Drugs.

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.

Cite this article as:

Haroun Michelyne*, Tratrat Christophe, Kositzi Katerina, Tsolaki Evangelia, Petrou Anthi, Aldhubiab Bandar, Attimarad Mahesh, Harsha Sree, Geronikaki Athina*, Venugopala N. Katharigatta , Elsewedy S. Heba, Sokovic Marina, Glamoclija Jasna and Ciric Ana, New Benzothiazole-based Thiazolidinones as Potent Antimicrobial Agents. Design, synthesis and Biological Evaluation, Current Topics in Medicinal Chemistry 2018; 18 (1) . https://dx.doi.org/10.2174/1568026618666180206101814