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New antibacterial cadiolide analogues active against antibiotic-resistant strains.

Authors :
Bekri S
Desriac F
Barreau M
Clamens T
Gallavardin T
Nahenec-Martel PL
Vieillard J
Datoussaid Y
Choukchou-Braham N
Lesouhaitier O
Franck X
Leleu S
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.)

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