Compositions of bifunctional inhibitors of tetracycline inactivating enzymes and methods of use thereof
AssigneeWashington University
InventorsTimothy Wencewicz, Gautam Dantas, Niraj Tolia, Emily Williford, Caitlin DeAngelo, Kevin Blake, Hirdesh Kumar
Life of this patent
Estimating the term…
Abstract
Among the various aspects of the present disclosure is the provision of bifunctional inhibitors of tetracycline inactivating enzymes and methods of use thereof. Herein, compositions for inhibitors of tetracycline inactivating enzymes are described. Additionally, a method of treatment for multidrug resistant bacterial infections using inhibitors of tetracycline inactivating enzymes is disclosed.
Claims16
A bisubstrate tetracycline destructase inhibitor compound comprising a C9-substituted anhydrotetracycline (aTC) analog, the C9-substituted anhydrotetracycline (aTC) analog comprising the structure:
- wherein R is selected from
- R Group
- 4
- 5
- 6
- 7
- 8
- 9
- 10
- 11
- 12
- 13
- 14
- 15
- 16
- 17
- 18
- 19
- 20
- 21
- .
A method of treating an infection with at least one of multidrug resistant (MDR) Gram-negative bacteria, extensively drug-resistant (XDR) Enterobacteriaceae species, and XDR Acinetobacter species, the method comprising administering, to a patient, a third-generation tetracycline in combination with a bisubstrate tetracycline destructase inhibitor compound.
Dependencies are inferred from the claim text.