Michelyne Haroun 1 , Christophe Tratrat 1 , Katerina Kositsi 2 , Evangelia Tsolaki 2 , Anthi Petrou 2 , Bandar Aldhubiab 1 , Mahesh Attimarad 1 , Sree Harsha 1 , Athina Geronikaki 2 , Katharigatta N Venugopala 1,3 , Heba S Elsewedy 1 , Marina Sokovic 4 , Jasna Glamoclija 4 , Ana Ciric 4 Show Affiliations »
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. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.
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. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.
Entities: Chemical
Disease
Keywords:
Antibacterial; Antifungal; Benzothiazole; Drugs.; Microdilution; Thiazolidinone
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Year: 2018
PMID： 29412109 DOI： 10.2174/1568026618666180206101814
Source DB: PubMed Journal: Curr Top Med Chem ISSN： 1568-0266 Impact factor: 3.295