Antimicrobial analogues of gramicidin S
Disclosed herein are N-aminated variants of Gramicidin S and methods of using the same for treating infections in a subject.
1. A compound of formula (I),
or a pharmaceutically acceptable salt thereof, wherein
R 1 , R 2 , R 3 , and R 4 are each independently selected from hydrogen or —NH 2 ; and
at least one of R 1 , R 2 , R 3 , and R 4 is —NH 2 .
2. The compound of claim 1 , wherein R 3 is —NH 2 .
3. The compound of claim 1 , wherein R 4 is —NH 2 .
4. The compound of claim 1 , wherein two of R 1 , R 2 , R 3 , and R 4 are —NH 2 .
5. The compound of claim 4 , wherein R 1 and R 3 are —NH 2 .
6. The compound of claim 4 , wherein R 3 and R 4 are —NH 2 .
7. The compound of claim 4 , wherein R 2 and R 3 are —NH 2 .
8. The compound of claim 4 , wherein R 2 and R 4 are —NH 2 .
9. The compound of claim 1 , wherein three of R 1 , R 2 , R 3 , and R 4 are —NH 2 .
10. The compound of claim 9 , wherein R 1 , R 3 and R 4 are —NH 2 .
11. The compound of claim 9 , wherein R 2 , R 3 and R 4 are —NH 2 .
12. The compound of claim 1 , wherein each of R 1 , R 2 , R 3 , and R 4 are —NH 2 .
13. A pharmaceutical composition comprising an effective amount of the compound of claim 1 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.
14. A method of treating an infection in a subject, comprising administering to the subject an effective amount of the pharmaceutical composition of claim 13 .
15. The method of claim 14 , wherein the infection is a fungal infection or a bacterial infection.
16. The method of claim 15 , wherein the infection is a gram-positive bacterial infection.
17. The method of claim 15 , wherein the infection is a gram-negative bacterial infection.
18. The method of claim 15 , wherein the infection is a multi-drug resistant infection.
19. The method of claim 14 , wherein the subject is a human.