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| Main Authors: | , , , , , , , |
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| Format: | Artículo científico |
| Language: | en |
| Published: |
Journal of natural products
2025
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| Subjects: | |
| Online Access: | https://pubmed.ncbi.nlm.nih.gov/40964850/ |
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Table of Contents:
- Design, Synthesis, and Antibacterial Activity of Long-Chain Alkyl-Substituted DemethyloxyAaptamine Derivatives. Liu, Yingqiu Wu, Wei Xue, Haitao Wang, Shu-Ping Xu, Jing Zhang, Tao Lin, Hou-Wen Liao, Hongze Anti-Bacterial Agents Microbial Sensitivity Tests Structure-Activity Relationship Staphylococcus aureus Molecular Structure Animals Drug Design Porifera Naphthyridines Vancomycin Demethyloxyaaptamine, isolated from the marine sponge , features a -benzo[][1,6]naphthyridine core and exhibits potent antibacterial activity. To systematically investigate its underexplored antibacterial properties and facilitate structural optimization, we constructed a focused library of 28 C-3 alkylamino-substituted derivatives of demethyloxyaaptamine via regioselective functionalization. evaluation against revealed that several derivatives possess minimum inhibitory concentrations (MICs) superior to vancomycin. Structure-activity relationship analysis (SAR) demonstrated that the incorporation of moderately hydrophobic alkylamino groups at the C-3 position markedly improved antimicrobial efficacy. Mechanistic investigations demonstrated that these compounds inhibit bacterial growth by targeting bacterial membrane. Together, these findings validate demethyloxyaaptamine as a privileged scaffold for targeting drug-resistant Gram-positive pathogens and deliver critical SAR insights to guide the design of next-generation antibiotics.