HYDROXAMIC ACIDS CONTAINING 1,2,4- AND 1,3,4-OXADIAZOLE NUCLEI AS POTENTIATORS OF ANTIBIOTIC ACTION Russian patent published in 2024 - IPC C07D271/06 C07D271/10 C07D271/107 A61K31/4245 A61P31/04 

FIELD: chemistry.

SUBSTANCE: invention relates to uridine diphosphate-3-O-(hydroxymyristoyl)-N-acetylglucosamine deacetylase (LpxC) enzyme inhibitors of formula (I) where A is 3,5-disubstituted nucleus of 1,2,4-oxadiazole (in the form of two regioisomers 1 and 2) or 2,5-disubstituted nucleus of 1,3,4-oxadiazole 3: B is a functional group of hydroxamic acid (C(O)NHOH), free or conjugated with an aliphatic or aromatic linker: R₁ is H, F, H₃CO, H₃C; R₂ is H, F, C1, I, H₃CO, H₃C; R₃ is H, F, C1, I, H₃CO, F₃CO; R₄ is H, F; R⁵ is H, F.

EFFECT: synthesis of new chemical compounds, which are inhibitors of the LpxC enzyme, having pharmacological activity, a decrease in the cytotoxicity of the synthesized chemical compounds, which are inhibitors of the LpxC enzyme, improvement of ADME-properties of synthesized chemical compounds, which are inhibitors of LpxC enzyme, is shown.

35 cl, 11 tbl, 99 ex, 13 dwg