Lipophosphonoxins of second generation, and their use

0519526 - ÚOCHB 2020 RIV eng P - Patent Document
Rejman, Dominik - Pohl, Radek - Zborníková, Eva - Krásný, Libor - Látal, T. - Kolář, M.
Lipophosphonoxins of second generation, and their use.
2019. Owner: Ústav organické chemie a biochemie AV ČR, v. v. i. - Mikrobiologický ústav AV ČR, v. v. i. - TRIOS, spol. s r. o. Date of the patent acceptance: 07.03.2019. Patent Number: AU2017257061
R&D Projects: GA TA ČR TA02010035
Institutional support: RVO:61388963 ; RVO:61388971
Keywords : antibacterial * lipophosphonoxin * chemotherapeutic
OECD category: Medicinal chemistry
https://worldwide.espacenet.com/publicationDetails/originalDocument?FT=D&date=20190307&DB=&locale=en_EP&CC=AU&NR=2017257061B2&KC=B2&ND=5#

Lipophosphonoxins of general Formula I are described here, wherein R1 is C8-C22, preferably C10-C18 and more preferably C12-C16 alkyl, or hexadecyloxypropyl, tetradecyloxypropyl, tetradecyloxyethyl or hexadecyloxyethyl, R2 is uracil, thymine, or cytosine, R3 is selected from a group which contains compounds of general formulas II and III, wherein R4 is H, CH2OH or CH2NH2, R5 is H, OH or NH2, R6 is H, OH or NH2, R7 is H, CH2OH or CH2NH2, wherein at least one of the groups R5 and R6 must be NH2 or one of the groups R4 and R7 must be CH2NH2. R8 is H, CH2OH or CH2NH2, R9 is H, OH or NH2, R10 is H, OH or NH2, R11 is H, OH or NH2, R12 is H, CH2OH or CH2NH2, wherein at least one of the groups R9, R10 and R11 must be NH2 or one of the groups R8 a R12 must be CH2NH2. R13 is NH2 or NH-CH(NH2)NH, R14 is NH2 or NH-CH(NH2)NH, R15 is NH2 or NH-CH(NH2)NH, R16 is NH2 or NH-CH(NH2)NH. Further, diastereomers and mixtures of diastereomers of compounds of general formula I and the corresponding pharmaceutically acceptable salts and/or hydrates are described. The compounds of general formula I are useful as antibacterial agents or active ingredients in disinfectants, and/or of selective in vitro culture media.
Permanent Link: http://hdl.handle.net/11104/0305037