Scaffold hopping in the oxadiazole antibiotic structure leads to more active compounds

[Display omitted] Isosteric replacement of the oxadiazole ring by amide bond in the structure of new non-β-lactam antibiotics led to compounds with higher activity against Gram-positive pathogens of ESKAPE panel. A series of 17 compounds were synthesized by acylation of 4-(4-fluorophenoxy)aniline wi...

Full description

Saved in:

Bibliographic Details
Published in:	Mendeleev communications Vol. 34; no. 3; pp. 362 - 364
Main Authors:	Vinogradova, Lyubov V., Komarova, Kristina Yu, Chudinov, Mikhail V., Rogacheva, Elizaveta V., Kraeva, Lyudmila A., Lukin, Alexey Yu
Format:	Journal Article
Language:	English
Published:	Elsevier B.V 01-05-2024
Subjects:	2,6-diazaspiro[3.4]octane antibiotic resistance carboxamides ESKAPE pathogens isosteric replacement methicillin-resistant bacteria non-β-lactam antibiotics organofluorine compounds ESKAPE pathogens isosteric replacement antibiotic resistance non-β-lactam antibiotics 2,6-diazaspiro[3.4]octane carboxamides organofluorine compounds methicillin-resistant bacteria
Online Access:	Get full text
Tags:	Add Tag No Tags, Be the first to tag this record!

Description
Summary:	[Display omitted] Isosteric replacement of the oxadiazole ring by amide bond in the structure of new non-β-lactam antibiotics led to compounds with higher activity against Gram-positive pathogens of ESKAPE panel. A series of 17 compounds were synthesized by acylation of 4-(4-fluorophenoxy)aniline with various amino acids. The spirocyclic derivative with 6-methylsulfonyl-2,6-diazaspiro[3.4]octane moiety showed excellent minimum inhibitory concentrations of 0.093–0.75 μg ml−1 against a number of methicillin-resistant Staphylococcus aureus strains.
ISSN:	0959-9436
DOI:	10.1016/j.mencom.2024.04.016