Literature DB >> 33253880

2-Aryl-3-(6-trifluoromethoxy)benzo[d]thiazole-based thiazolidinone hybrids as potential anti-infective agents: Synthesis, biological evaluation and molecular docking studies.

Michelyne Haroun1, Christophe Tratrat2, Anthi Petrou3, Athina Geronikaki4, Marina Ivanov5, Ana Ciric5, Marina Sokovic5.   

Abstract

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.
Copyright © 2020 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Ampicillin; Antibacterial; Benzothiazole; MurB; Thiazolidinone

Year:  2020        PMID: 33253880     DOI: 10.1016/j.bmcl.2020.127718

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

Review 1.  The Bioactivity of Thiazolidin-4-Ones: A Short Review of the Most Recent Studies.

Authors:  Dominika Mech; Antonina Kurowska; Nazar Trotsko
Journal:  Int J Mol Sci       Date:  2021-10-26       Impact factor: 5.923

2.  A Novel PIFA/KOH Promoted Approach to Synthesize C2-arylacylated Benzothiazoles as Potential Drug Scaffolds.

Authors:  Xiao-Tong Sun; Zhi-Gang Hu; Zhen Huang; Ling-Li Zhou; Jian-Quan Weng
Journal:  Molecules       Date:  2022-01-22       Impact factor: 4.411

  2 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.