Antibiotic compositions and methods of use
Inventors
Turos, Edward • Bhattacharya, Biplob
Assignees
University of South Florida • University of South Florida St Petersburg
Publication Number
US-9670179-B1
Publication Date
2017-06-06
Expiration Date
2034-03-13
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Abstract
Embodiments of the present disclosure provide for compositions including an antibiotic containing a N-thiolated beta-lactam moiety, pharmaceutical compositions including the antibiotic, methods of treatment of a condition (e.g., bacterial infection), methods of treatment using compositions or pharmaceutical compositions, and the like.
Core Innovation
The invention provides compositions comprising an antibiotic that contains an N-thiolated beta-lactam moiety. These include standalone N-thiolated beta-lactam antibiotics as well as pharmaceutical compositions where the antibiotic can be present in a therapeutically effective amount or as a pharmaceutically acceptable salt, combined with a suitable carrier, and are intended for treating conditions such as bacterial infections.
The invention addresses the urgent problem of drug-resistant bacterial pathogens and the decline in discovery and approval of new antibacterial agents. The background emphasizes a critical need for sustainable development of new antibacterial drugs capable of overcoming present resistance trends and anticipating future resistance.
The core innovation also extends to methods of treating bacterial infections by delivering the N-thiolated beta-lactam-containing antibiotics or their pharmaceutical compositions to subjects in need. The disclosure details the chemical structures of these antibiotics, including variations in aryl and aliphatic substituents, possible prodrug forms, and the possibility of attaching other antibiotic agents to the N-thiolated beta-lactam via cleavable linkages.
Claims Coverage
There are two independent claims in the patent, covering the primary composition and a pharmaceutical composition containing N-thiolated beta-lactam antibiotics.
Composition comprising an antibiotic containing a N-thiolated beta-lactam moiety
- The composition includes an antibiotic with a specific N-thiolated beta-lactam moiety, represented by structure A. - Structure A defines AA as an antimicrobial agent; R' as a substituted or unsubstituted aryl moiety; R as a substituted or unsubstituted, linear or branched, aliphatic moiety or a substituted or unsubstituted aryl moiety.
Pharmaceutical composition comprising a therapeutically effective amount of an antibiotic containing the N-thiolated beta-lactam moiety and a pharmaceutically acceptable carrier
- A pharmaceutical composition contains a therapeutically effective amount of an antibiotic with the N-thiolated beta-lactam moiety (structure A) or its pharmaceutically acceptable salt. - Includes a pharmaceutically acceptable carrier. - Intended to treat bacterial infection.
The inventive features claim both the composition of N-thiolated beta-lactam antibiotics and their use in pharmaceutical preparations for treating bacterial infections.
Stated Advantages
Embodiments can be bactericidal and/or bacteriostatic, meaning they can kill bacteria and/or inhibit bacterial growth.
The invention provides therapeutic options for treating infections caused by drug or multidrug resistant bacteria.
Dual-action antibiotics with different pharmacotherapeutic profiles may address bacterial resistance more effectively than a single drug.
Documented Applications
Treatment of bacterial infections in humans and animals using compositions or pharmaceutical compositions containing antibiotics with N-thiolated beta-lactam moieties.
Use in treating infections caused by drug or multidrug resistant bacteria, including pathogens such as Staphylococcus aureus, Streptococcus pyogenes, Streptococcus pneumonia, Enterococcus faecalis, Enterococcus faecium, Pseudomonas aeruginosa, Clostridium difficile, Escherichia coli, Salmonella, Acinetobacter baumannii, and Mycobacterium tuberculosis.
Prophylactic administration to subjects at risk of bacterial infection.
Formulation into a variety of pharmaceutical forms such as oral tablets, capsules, powders, injections, aerosols, suppositories, or as part of continuous or controlled delivery systems (e.g., pumps, implantable devices).
Impregnation or coating of medical devices, sutures, bandages, gauze, surgical staples, zippers, and catheters for delivery of the antibiotic.
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