Reducing tetracycline resistance in living cells
AssigneeTrustees of Tufts College
InventorStuart B. Levy
Life of this patent
Estimating the term…
Loading patent…
AssigneeTrustees of Tufts College
InventorStuart B. Levy
Estimating the term…
The present invention provides an improved methodology by which therapeutically to overcome resistance to tetracycline in living cells including bacteria, parasites, fungi, and rickettsiae. The methodology employs a blocking agent such as C5 ester derivatives, or 13-(substituted mercapto) derivatives of tetracycline, in combination with other tetracycline-type antibiotics as a synergistic combination of compositions to be administered simultaneously, sequentially or concurrently. In another embodiment, C5 ester novel compositions are provided which may be administered alone against, for example, a sensitive or resistant strain of gram positive bacteria such as S. aureus and E. faecalis. The concomitantly administered compositions effectively overcome the tetracycline resistant mechanisms present such that the cell is effectively converted from a tetracycline-resistant state to a tetracycline-sensitive state.
A pharmaceutical composition for converting tetracycline resistant bacteria into tetracycline sensitive bacteria comprising a C5 ester of tetracycline and a tetracycline-type antibiotic which is not a C5 ester of tetracycline, and a pharmaceutically acceptable carrier.
A pharmaceutical composition for converting tetracycline resistant bacteria into tetracycline sensitive bacteria comprising a 13,5 derivative of tetracycline and a tetracycline-type antibiotic which is not a 13,5 derivative of tetracycline, and a pharmaceutically acceptable carrier.
C5 esters having the formula ##STR22## wherein R.sub.1 and R.sub.2 are selected from the group consisting of a methylene group, hydroxyl, hydrogen or a group consisting of organic entities comprising from 1-12 carbon atoms, with or without other heteroatoms including sulfur, oxygen, halogen, nitrogen, and the like, and takes form as linear, branched, or cyclic alkyl, aryl, or alkylaryl structures;
A compound of the following formula ##STR23## where R is an organic entity comprising 1-12 carbon atoms and optionally including one or more heteroatoms or halogen atoms;
A method for converting tetracycline resistant bacteria into tetracycline sensitive bacteria, comprising contacting the resistant bacteria with a predetermined quantity of at least a first composition selected from C5 esters of tetracycline or a 13,5 derivative of tetracycline, and concomitantly administering to the cell a predetermined quantity of at least a second composition selected from a tetracycline, a tetracycline analogue or a tetracycline derivative which is not a C5 ester of tetracycline nor a 13,5 derivative of tetracycline.
A method for exerting cidal activity against susceptible bacteria, comprising:
A method for therapeutically treating tetracycline sensitive or resistant bacteria, comprising:
Dependencies are inferred from the claim text.