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 

Abstract RU 2830361 C1

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

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RU 2 830 361 C1

Authors

Chernyshov Vladimir Vladimirovich

Zhukovets Anastasiia Alekseevna

Almukhametov Aidar Zufarovich

Mitkevich Vladimir Aleksandrovich

Dates

2024-11-18Published

2023-12-08Filed