Synthesis of Degraded Limonoid Analogs as New Antibacterial Scaffolds against Staphylococcus aureus

Staphylococcus aureus and methicillin-resistant Staphylococcus aureus (MRSA) have become serious infections in humans and ruminants. S. aureus strains are showing rapid changes to develop resistance in traditional antibiotic-containing systems. In the continuous fierce fight against the emergent mul...

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Bibliographic Details
Published in:Antibiotics (Basel) 2020-08, Vol.9 (8), p.488
Main Authors: Ferrera-Suanzes, Marta, Prieto, Victoria, Medina-Olivera, Antonio J., Botubol-Ares, José Manuel, Galán-Sánchez, Fátima, Rodríguez-Iglesias, Manuel A., Hernández-Galán, Rosario, Durán-Peña, María Jesús
Format: Article
Language:English
Subjects:
Analogs
Antibiotics
Antiinfectives and antibacterials
Antimicrobial agents
Bacteria
Bioavailability
Chromatography
Degradation
degraded limonoids
Demand analysis
drug design
Drug resistance
drug-like properties
Gram-positive bacteria
Health aspects
Hydrogen bonds
Limonoids
Mass spectrometry
Metabolites
Methicillin
Molecular weight
MRSA
Multidrug resistance
Multidrug resistant organisms
Pharmaceutical industry
Prevention
S. aureus
Scaffolds
Scientific imaging
Staphylococcus aureus
Staphylococcus infections
Stereoisomerism
Stereoisomers
Strains (organisms)
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Summary:Staphylococcus aureus and methicillin-resistant Staphylococcus aureus (MRSA) have become serious infections in humans and ruminants. S. aureus strains are showing rapid changes to develop resistance in traditional antibiotic-containing systems. In the continuous fierce fight against the emergent multi-drug resistant bacterial strains, straightforward and scalable synthetic procedures to produce new active molecules are in demand. Analysis of molecular properties points to degraded limonoids as promising candidates. In this article, we report a simple synthetic approach to obtain degraded limonoid analogs as scaffolds for new antibacterial molecules. The minimum inhibitory concentrations against S. aureus were evaluated for the stereoisomer mixtures by the broth microdilution method. Analysis of results showed that the acetylated derivatives were the most active of them all.
ISSN:2079-6382
2079-6382
DOI:10.3390/antibiotics9080488