Lipophosphonoxins, their preparation and use
Lipophosphonoxins of general formula I, diastereomers and mixtures of diastereomers of compounds of general formula I and their pharmaceutically acceptable salts and hydrates as antibacterial agents, forming an active ingredient in pharmaceutical compositions for the treatment of resistant bacterial infections, disinfectants and/or selective culture media is disclosed.
1 . A lipophosphonoxin of the general formula I
wherein:
the X substituent is independently selected from the following structures:
wherein m=1-3;
the Y1 and Y2 substituents are independently selected from the following structures:
wherein n=0-12, and o=0-12, and p=0-12, and
R 1 , R 2 , R 3 , R 4 , and R 5 are independently selected from the group consisting of: H—, CH 3 —, CH 2 CH 3 , propyl, isopropyl, isobutyl, tert-butyl, CH 3 O—, CH 2 CH 3 O—, propoxy, isopropoxy, isobutyloxy or tert-butyloxy; and
the Z substituent is selected from the following structures:
wherein q=2-14, and r=0-10, and s=0-10,
or a diastereomer or a mixture of diastereomers of the lipophosphonoxin of formula I, or a pharmaceutically acceptable salt or hydrate thereof.
2 . A method of administering a medicament, comprising a step of administering lipophosphonoxin of general formula I according to claim 1 or a diastereomer or a pharmaceutically acceptable salt or hydrate thereof to a subject in need thereof.
3 . A method of administering an antibacterial drug comprising a step of administering lipophosphonoxin of general formula I according to claim 1 or a diastereomer or a pharmaceutically acceptable salt or hydrate thereof to a subject in need thereof.
4 . An antibacterial drug comprising at least one lipophosphonoxin of general formula I as claimed in claim 1 , or a diastereomer or a pharmaceutically acceptable salt or hydrate thereof.
5 . A disinfectant for non-therapeutic purposes comprising at least one lipophosphonoxin of general formula I as claimed in claim 1 , or a diastereomer or a pharmaceutically acceptable salt or hydrate thereof as active ingredient.
6 . A selective culture medium comprising at least one lipophosphonoxin of general formula I as claimed in claim 1 , or a diastereomer or a pharmaceutically acceptable salt or hydrate thereof as active ingredient.
7 . A method of treatment of bacterial infections, said method comprising a step of administering at least one lipophosphonoxin of the general formula I as claimed in claim 1 , or diastereomer or a pharmaceutically acceptable salt or hydrate thereof to a subject in need of such treatment.