Synthesis and antibacterial activity of 5-methoxy- and 5-hydroxy-6-fluoro-1,8-naphthyridone-3-carboxylic acid derivatives.

doi:10.1016/J.BMCL.2005.04.007

Paper

Synthesis and antibacterial activity of 5-methoxy- and 5-hydroxy-6-fluoro-1,8-naphthyridone-3-carboxylic acid derivatives.

Published Jun 2, 2005 · T. Matthew Hansen, Y. Gu, Tamara M Rehm

Bioorganic & medicinal chemistry letters

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6

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Abstract

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In Vitro Study

Study Snapshot

5-methoxy and 5-hydroxy-6-fluoro-1,8-naphthyridone-3-carboxylic acid derivatives show moderate whole cell antibacterial activity, with the 5-OH group negatively impacting biochemical potency.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Synthesis and antibacterial activity of 5-methoxy- and 5-hydroxy-6-fluoro-1,8-naphthyridone-3-carboxylic acid derivatives.

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References

Novel inhibitors of bacterial protein synthesis: structure-activity relationships for 1,8-naphthyridine derivatives incorporating position 3 and 4 variants.

The novel ribosome inhibitors (NRI) show potential as antibacterials due to their potent protein synthesis inhibitory activity and potential for improved cellular penetration.

A Strategy for Discovery of Novel Broad-Spectrum Antibacterials Using a High-Throughput Streptococcus pneumoniae Transcription/Translation Screen

A high-throughput screen for Streptococcus pneumoniae transcription/translation inhibitors identified a novel broad-spectrum antibiotic with selectivity against mammalian biochemical and whole-cell assays.

Novel Antibacterial Class

The novel ribosome inhibitor (NRI) class exhibits selective and broad-spectrum antibacterial activity against common respiratory pathogens, with potential for future antibacterial treatments.

The future challenges facing the development of new antimicrobial drugs

Targeting non-multiplying latent bacteria in antibacterial drug development could potentially alleviate drug resistance and improve human health.

Fluoroquinolone Resistance in Streptococcus pneumoniae in United States since 1994-1995

No significant changes in fluoroquinolone activity or resistance rates were observed in Streptococcus pneumoniae strains over a 5-year period (1994-1995 through 1999-2000).

Citations

Coumarins as Fungal Metabolites with Potential Medicinal Properties

Fungal coumarins show potential medicinal properties, with potential applications in cancer, neuronal injury, microbial and parasitic infections, and biomedical engineering.

Synthesis and characterization of some bi, tri and tetravalent transition metal complexes of N'-(furan-2-yl-methylene)-2-(p-tolylamino)acetohydrazide HL1 and N'-(thiophen-2-yl-methylene)-2-(p-tolylamino)acetohydrazide HL2.

Transition metal complexes with ligands HL1 and HL2 show weak antimicrobial activity against tested microorganisms.

Synthesis and antibacterial activities of new quinolone derivatives utilizing 1-azabicyclo[1.1.0]butane.

New quinolone derivatives utilizing 1-azabicyclo[1.1.0]butane show promising antibacterial activity against quinolone-susceptible MRSA compared to currently used fluoroquinolones.

Fluoroquinolones: Synthesis and Application

Fluoroquinolones show promising antibacterial activity and other biological activities, with potential applications in various fields.

DNA-GYRASE: A POTENTIAL AND EMERGING TARGET FOR FINDING NOVEL ANTI-BACTERIAL AGENTS

DNA-gyrase is a potential target for developing novel antibacterial agents against multi-drug resistant strains, as resistance to current antibiotics poses a major challenge in antibiotic research.