IP Library Granted Patent US 11,103,504
Granted Patent B2
US 11,103,504 · App. 16/518,736 · Granted Aug 31, 2021

Combination of a DNA condensation-inducing compound and an Eis inhibitor for antibiotic treatment

Inventors: Sylvie Garneau-Tsodikova (Lexington, KY); Nicole Neeltje van der Wel (Amsterdam, NL)
Assignees: University of Kentucky Research Foundation; Academisch Medisch Centrum
A61K31/4985A61K31/4375A61K31/496A61K31/5377A61K31/575A61K31/7036A61P31/06
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Quick Facts
Patent No.
US 11,103,504
App. No.
16/518,736
Granted
Aug 31, 2021
Kind
B2
Abstract

A method of killing bacteria and an antibiotic kit are provided herein. The method includes treating the bacteria with a DNA condensation-inducing compound; and subsequently treating the bacteria with an Eis inhibitor. The kit includes a DNA condensation-inducing compound packaged together with an Eis inhibitor.

Claims (26)

1. A method of killing bacteria, comprising:

treating the bacteria with a DNA condensation-inducing compound; and

subsequently treating the bacteria with an Eis inhibitor.

2. The method of claim 1 , wherein the DNA condensation-inducing compound is an antibiotic.

3. The method of claim 2 , wherein the antibiotic is selected from the group consisting of: fusidic acid, nalidixic acid, linezolid, streptomycin, and rifampicin.

4. The method of claim 1 , wherein the Eis inhibitor is a pyrrolo[1,5-a]pyrazine-based Eis inhibitor having the following structure:

wherein R 1 is selected from the group consisting of H, p-F, and m,p-di-F; and

wherein R 2 is selected from the group consisting of H, o-F, m-F, p-F, m-Cl, p-Cl, m-Br, p-Br, p Me, and m-OMe.

5. The method of claim 1 , wherein the bacteria are mycobacteria.

6. The method of claim 1 , wherein the bacteria include Mycobacterium tuberculosis.

7. The method of claim 1 , wherein the bacteria include Mycobacterium smegmatis.

8. The method of claim 1 , wherein the bacteria are causing an infection in a subject.

9. The method of claim 8 , wherein the step of treating the bacteria with a DNA condensation-inducing compound includes administering the DNA condensation-inducing compound to the subject.

10. The method of claim 9 , wherein the step of subsequently treating the bacteria with the Eis inhibitor includes administering the Eis inhibitor to the subject.

11. An antibiotic kit, comprising: a DNA condensation-inducing compound packaged together with an Eis inhibitor.

12. The kit of claim 11 , wherein the DNA condensation-inducing compound is an antibiotic.

13. The kit of claim 12 , wherein the antibiotic is selected from the group consisting of: fusidic acid, nalidixic acid, linezolid, streptomycin, and rifampicin.

14. The kit of claim 11 , wherein the Eis inhibitor is a pyrrolo[1,5-a]pyrazine-based Eis inhibitor having the following structure:

wherein R 1 is selected from the group consisting of H, p-F, and m,p-di-F; and

wherein R 2 is selected from the group consisting of H, o-F, m-F, p-F, m-Cl, p-Cl, m-Br, p-Br, p Me, and m-OMe.

15. The kit of claim 11 , further comprising instructions for killing bacteria.

16. The kit of claim 15 , wherein the bacteria are mycobacteria.

17. The kit of claim 15 , wherein the bacteria include Mycobacterium tuberculosis.

18. The kit of claim 15 , wherein the bacteria include Mycobacterium smegmatis.

19. The kit of claim 15 , wherein the bacteria are causing an infection in a subject.

20. The kit of claim 15 , wherein the instructions comprise administering the DNA condensation-inducing compound to the subject, and subsequently administering the Eis inhibitor to the subject.

Assignments (3)
CHANGE OF NAME Recorded Sep 11, 2024
From: ACADEMISCH MEDISCH CENTRUM
To: STICHTING AMSTERDAM UMC
Reel/Frame 068942/0762 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 22, 2019
From: GARNEAU-TSODIKOVA, SYLVIE
To: UNIVERSITY OF KENTUCKY RESEARCH FOUNDATION
Reel/Frame 049824/0222 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 22, 2019
From: VAN DER WEL, NICOLE N
To: ACADEMISCH MEDISCH CENTRUM
Reel/Frame 049824/0310 →
Continuity (2)
Provisional Application 62701373 · Jul 20, 2018
Related Publication 20200022978A1 · Jan 23, 2020