Anti-infective agents

• Main Authors: Norman B Roberts, Lakshminarayan Ranganath, Nicolas Thierry Sireau, James A Gallagher, George Bou-Gharios
• Format: Patent
• Language: English
• Published: 08.12.2021
• Subjects: BEER; BIOCHEMISTRY; CHEMISTRY; COMPOSITIONS OR TEST PAPERS THEREFOR; COMPOSITIONS THEREOF; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL ORENZYMOLOGICAL PROCESSES; CULTURE MEDIA; ENZYMOLOGY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEICACIDS OR MICROORGANISMS; MEDICAL OR VETERINARY SCIENCE; METALLURGY; MICROBIOLOGY; MICROORGANISMS OR ENZYMES; MUTATION OR GENETIC ENGINEERING; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; PROCESSES OF PREPARING SUCH COMPOSITIONS; PROPAGATING, PRESERVING OR MAINTAINING MICROORGANISMS; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS; SPIRITS; VINEGAR; WINE

The benefit of inhibiting the activity of the enzyme homogentisate 1, 2 dioxygenase when homogentisic acid is used as an antibacterial agent is disclosed. Inhibitors of homogentisate 1, 2 dioygenase (HGD) such as homogentisic acid derivatives of formula 1 (wherein: R1 is H, OH, or a halogen; R2 is H, OH, C1 to C4 linear or branched alkyl, or a halogen; R3 is H, OH, or a halogen; R3 is H, OH, or a halogen; and X is -CH2- or -CH2CH2-) and inhibitory antisense nucleic acids such as siRNA that can reduce mRNA translation and preferably has at least 80% sequence identity to the full antisense cDNA or mRNA sequences of HGD are disclosed. The combined therapeutic use of homogentisic acid (HGA) with an inhibitor of homogentisate 1, 2 dioxygenase is disclosed alongside methods for the screening for suitable homogentisate 1, 2 dioxygenase inhibitors.