Antibacterial agents: phloroglucinol derivatives
View Patent ↗The invention provides a compound of formula I: or a salt thereof, wherein R 1 -R 3 have any of the values described in the specification, as well as compositions comprising a compound of formula I. The compounds are useful as antibacterial agents.
1. A compound of formula I:
wherein:
R 1 is H, Cl, Br, I, (C 1 -C 6 )alkyl, optionally substituted by halogen, or (C 1 -C 6 )alkoxy, optionally substituted by halogen;
R 2 is H, halogen, trifluoromethyl, (C 2 -C 6 )alkyl, optionally substituted by halogen, or (C 1 -C 6 )alkoxy, optionally substituted by halogen; and
R 3 is H, halogen, trifluoromethyl, (C 2 -C 6 )alkyl, optionally substituted by halogen, or (C 2 -C 6 )alkoxy, optionally substituted by halogen;
provided that at least one of R 1 , R 2 , or R 3 is not H;
or a salt thereof.
2. The compound of claim 1 , which is
or a salt thereof.
3. A composition comprising a compound of formula I as described in claim 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable vehicle.
4. A method for inhibiting a bacterial RNA polymerase comprising contacting the bacterial RNA polymerase with a compound of formula I as described in claim 1 , or a salt thereof.
5. A method for inhibiting the growth of a bacterium comprising contacting the bacterium with a compound of formula I as described in claim 1 , or a salt thereof.
6. A method for treating a bacterial infection selected from Mycobacterium tuberculosis, Staphylococcus aureus MSSA and MRSA, Enterococcus faecalis, Enterococcus faecium, Bacillus anthracis, Escherichia coli, Haemophilus influenzae, Moraxella catarrhalis, Francisella tularensis or Burkholderia mallei in a mammal comprising administering to the mammal an effective amount of a compound of formula I as described in claim 1 , or a pharmaceutically acceptable salt thereof.
7. The composition of claim 3 , in the form of a disinfectant, sterilant, antispoilant, or antiseptic.
8. A composition comprising a compound of formula I as described in claim 2 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable vehicle.
9. The composition of claim 8 , in the form of a disinfectant, sterilant, antispoilant, or antiseptic.
10. A method for treating a bacterial infection selected from Mycobacterium tuberculosis, Staphylococcus aureus MSSA and MRSA, Enterococcus faecalis, Entercoccus faecium, Bacillus anthracis, Escherichia coli, Haemophilus infuenzae, Moraxella catarrhalis, Francisella tularensis or Burkholderia mallei in a mammal comprising administering to the mammal an effective amount of a compound of formula I as described in claim 2 , or a pharmaceutically acceptable salt thereof.
11. A method for inhibiting a bacterial RNA polymerase comprising contacting the bacterial RNA polymerase with a compound of formula I as described in claim 2 , or a salt thereof.
12. A method for inhibiting the growth of a bacterium comprising contacting the bacterium with a compound of formula I as described in claim 2 , or a salt thereof.
13. A compound of formula I:
wherein:
R 1 is H, Cl, Br, I, (C 1 -C 6 )alkyl, optionally substituted by halogen, or (C 1 -C 6 )alkoxy, optionally substituted by halogen;
R 2 is H, Cl, Br, I, trifluoromehtyl, (C 2 -C 6 )alkyl, optionally substituted by halogen, or (C 1 -C 6 )alkoxy, optionally substituted by halogen;
R 3 is H, halogen, trifluoromethyl, (C 2 -C 6 )alkyl, optionally substituted by halogen, or (C 2 -C 6 )alkoxy, optionally substituted by halogen;
provided that at least one of R 1 , R 2 , or R 3 is not H;
or a salt thereof.
14. The compound of claim 13 , provided that at least one of R 1 or R 3 is H.