2-Aryl-3-(6-trifluoromethoxy)benzo[d]thiazole-based thiazolidinone hybrids as potential anti-infective agents: Synthesis, biological evaluation and molecular docking studies.
Anti-Infective Agents
/ chemical synthesis
Bacterial Proteins
/ antagonists & inhibitors
Binding Sites
Carbohydrate Dehydrogenases
/ antagonists & inhibitors
Gram-Negative Bacteria
/ drug effects
Gram-Positive Bacteria
/ drug effects
Isomerism
Microbial Sensitivity Tests
Molecular Docking Simulation
Thiazoles
/ chemistry
Thiazolidines
/ chemistry
Ampicillin
Antibacterial
Benzothiazole
MurB
Thiazolidinone
Journal
Bioorganic & medicinal chemistry letters
ISSN: 1464-3405
Titre abrégé: Bioorg Med Chem Lett
Pays: England
ID NLM: 9107377
Informations de publication
Date de publication:
15 01 2021
15 01 2021
Historique:
received:
12
10
2020
revised:
03
11
2020
accepted:
22
11
2020
pubmed:
1
12
2020
medline:
11
8
2021
entrez:
30
11
2020
Statut:
ppublish
Résumé
The search for new antimicrobial agents is greater than ever due to the perpetual threat of multidrug resistance in known pathogens and the relentless emergence of new infections. In this manuscript, ten thiazole-based thiazolidinone hybrids bearing a 6-trifluoromethoxy substituent on the benzothiazole core were synthesized and evaluated against a panel of four bacterial strains Salmonella typhimurium, Staphylococcus aureus, Escherichia coli and Listeria monocytogenes and three resistant strains Pseudomonas aeruginosa, E. coli and MRSA. The evaluation of minimum bactericidal and minimum inhibitory concentrations was accomplished by microdilution assay. As reference compounds ampicillin and streptomycin were employed. All compounds displayed antibacterial efficiencies with MBCs/MICs at 0.25-1 mg/mL and 0.12-1 mg/mL respectively while ampicillin displayed MBCs/MICs at 0.15-0.3 mg/mL and at 0.1-0.2 mg/mL respectively. MICs/MBC of streptomycin varied from 0.05 to 0.15 mg/mL and from 0.1 to 0.3 mg/mL respectively. The best overall effect was observed for compound h4, while compound h1 exhibited the highest effective action against E. coli (MIC/MBC 0.12/0.25 mg/ml) among all tested compounds.
Identifiants
pubmed: 33253880
pii: S0960-894X(20)30829-5
doi: 10.1016/j.bmcl.2020.127718
pii:
doi:
Substances chimiques
Anti-Infective Agents
0
Bacterial Proteins
0
Thiazoles
0
Thiazolidines
0
Carbohydrate Dehydrogenases
EC 1.1.-
UDP-N-acetylmuramate dehydrogenase
EC 1.3.1.98
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
127718Informations de copyright
Copyright © 2020 Elsevier Ltd. All rights reserved.