Eis inhibitors
AssigneeUniversity of Kentucky Research Foundation
InventorsSylvie Garneau-Tsodikova, Oleg V. Tsodikov, James E. Posey
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Abstract
Provided herein are novel small-molecules that have use in the inhibition of Eis, which mediates kanamycin resistance in Mycobacterium tuberculosis. The presently-disclosed subject matter further includes a pharmaceutical composition including a small molecule inhibitor, as described herein, and a suitable pharmaceutical carrier. Methods of treating tuberculosis comprising administering to an individual an effective amount of the disclosed small molecule inhibitors to mediate kanamycin A resistance and treat tuberculosis are also provided.
Claims16
A compound of the formula:
- wherein R is selected from the group consisting of
A method of inhibiting Eis comprising administering an effective amount of a composition comprising a compound according to the formula:
- wherein
- R1 is selected from:
- R2 is selected from:
- and
- when R1 is
- R2 is
- when R1 is
- R2 is
- when R1 is
- R2 is
- when R1 is
- R2 is
- when R1 is
- R2 is
- when R1 is
- R2 is
- when R1 is
- R2 is
- when R1 is
- R2 is
- and
- when R1 is
- R2 is —NH(CH2)3N(CH2CH3)2,
Dependencies are inferred from the claim text.