Albicidin Derivatives, Their Use and Synthesis

Simple SummaryContent extracted from patent full text and abstract with AI.

This patent discloses a new class of antibiotic compounds called albicidin derivatives. These molecules are structurally related to natural albicidin (originally discovered from a sugarcane pathogen) but have been modified by chemical synthesis to enhance their antibacterial activity, spectrum, or pharmacological properties. Detailed methods for their synthesis, structural variations, and formulations are described. The compounds, available as individual enantiomers or mixtures, display potent activity—especially against Gram-negative and Gram-positive bacteria, including drug-resistant strains—and are developed for pharmaceutical use in treating bacterial infections.

Use CasesContent extracted from patent full text and abstract with AI.

• Therapeutic agents for treating infections caused by Gram-negative bacteria, such as Escherichia coli, Salmonella, Pseudomonas aeruginosa, and Klebsiella pneumoniae.
• Treatment of infections determined to be resistant to existing antibiotics, including fluoroquinolones like ciprofloxacin.
• Infection control in hospital settings, particularly where prevalence of multidrug-resistant bacteria is high (e.g., ESKAPE pathogens).
• Possible use as topical antibacterials for skin infections, ointments, or sprays for wound healing.
• Development as oral, intravenous, or inhaled treatments for systemic or localized infections (lung, urinary tract, gastrointestinal, etc.).
• Veterinary applications for bacterial infections in animals.

BenefitsContent extracted from patent full text and abstract with AI.

• Effective against both Gram-negative and Gram-positive bacteria, expanding the spectrum over many current antibiotics.
• Demonstrates activity against bacteria that are resistant to common antibiotics, providing an option for hard-to-treat infections.
• Synthetic versatility allows tailoring of the molecular structure for optimal pharmacological properties, such as stability, solubility, and bioavailability.
• Use of specific enantiomers or enantiomeric mixtures may optimize efficacy and reduce potential side effects.
• Detailed synthesis pathways support scalable production—important for pharmaceutical manufacturing.
• Options for high-purity pharmaceutical preparations enable safer and more reliable dosing.
• Potential to address critical medical needs posed by antibiotic resistance.

Technical Classifications (CPCs)

Inventors & Applicants

Patent Abstract

The present invention relates to a antibiotically active compounds characterized by general formula (I), wherein X1, BB, BC, BD, BE and X2 are building blocks with D1, D2, D3, D4 or D5 being linkers which comprise carbon, sulphur, nitrogen, phosphor and/or oxygen atoms and which are covalently connecting the moities BA and BB, BB and BC, BC and BD, BD and BE and BE and BF, respectively, and wherein in particular the building block BC comprises an amino acid derivative. The invention relates further to said compounds for use in a method of treatment of diseases, in particular for use in a method of treatment of bacterial infections.