C11674: Novel Beta-Lactamase Inhibitors
Novelty:
This technology comprises of a series of compounds based on a novel scaffold that selectively inhibits the enzyme, beta lactamase with high affinity thereby providing a potential solution to beta-lactam resistance in bacteria.
Value Proposition:
Development of resistance to currently available beta-lactam antibiotics in bacteria is a major infectious diseases and public health problem. This technology provides a family of compounds based on a novel chemical scaffold that can combat beta lactamase resistance in bacteria. Other advantages include:
• Compounds display a high affinity for beta lacatamase enzyme
• Low molecular weight compounds with a non beta-lactam backbone.
• The new scaffold is easily modifiable and may be applicable to treat Gram-positive and Gram-negative infections.
• Potential to be combined with a range of currently available beta-lactam antibiotics.
Technical Details:
Johns Hopkins researchers have synthesized compounds with a non-beta lactam based scaffold to inhibit beta lactamase enzyme. Beta lactam antibiotics, like penicillin, cephamycin, and carbapenem incorporate a four-atom ring that gives these agents their antibacterial properties. The lactamase enzyme breaks that ring open and deactivates these antibiotics thereby conferring resistance to the bacterium. At the clinical level, the class A (TEM) and class C (AmpC) enzymes are the most important beta lactamases. Specifically, several derivatives of a small molecular weight, non-peptidic, non-beta-lactam scaffold were synthesized that block wild type TEM-1 beta lactamase, mutants associated with drug resistance, and AmpC beta lactamases. Several configurations were proposed and several moieties were particularly effective in decreasing the activity of the enzymes. Given that there have been a growing number of bacteria evolving resistance mechanisms against beta lactamase inhibitors; the use of a family of therapeutic drugs that are more potent will be extremely valuable.
Looking for Partners:
To develop and commercialize the technology as an anti-infective bacterial agent, to treat microorganism strains displaying beta-lactam resistance.
Stage of Development:
Pre-Clinical
Data Availability:
Under CDA / NDA
Publications/Associated Cases:
