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New antibacterial cadiolide analogues active against antibiotic-resistant strains.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2020 Nov 01; Vol. 30 (21), pp. 127580. Date of Electronic Publication: 2020 Sep 25. - Publication Year :
- 2020
-
Abstract
- The synthesis of new cadiolide analogues was carried out using a one-pot multi component synthesis. The antibacterial activity of these molecules was evaluated on standard and antibiotic resistant bacterial strains chosen for their involvement in human health or in food-born poisoning. Four molecules have shown good activities with MICs of 2 μg/mL <superscript>-1</superscript> . The introduction of an indole group or the conversion of the lactone into lactam have highlighted two new families of molecules with promising antibacterial activity. In addition, most of these active molecules are devoid of cytotoxic activity against keratinocyte cells.<br />Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.<br /> (Copyright © 2020 Elsevier Ltd. All rights reserved.)
- Subjects :
- 4-Butyrolactone chemical synthesis
4-Butyrolactone chemistry
Anti-Bacterial Agents chemical synthesis
Anti-Bacterial Agents chemistry
Biofilms drug effects
Dose-Response Relationship, Drug
Humans
Microbial Sensitivity Tests
Molecular Structure
Structure-Activity Relationship
4-Butyrolactone pharmacology
Anti-Bacterial Agents pharmacology
Drug Resistance, Bacterial drug effects
Gram-Negative Bacteria drug effects
Gram-Positive Bacteria drug effects
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 30
- Issue :
- 21
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 32987133
- Full Text :
- https://doi.org/10.1016/j.bmcl.2020.127580