Kamenetskaya O.L.”Synthesis of biologically active compounds in series of derivatives of 2-oxo-4-hydroxyquinolin-3-acetic acid”. – Manuscript.
The thesis for Ph.D. (Pharmacy), speciality 15.00.02. – Pharmaceutical chemistry and pharmacognosy. – National Ukrainian Academy of Pharmacy, Kharkiv, 2001.
Biologically active derivatives of 1H-2-oxo-4-hydroxyquinolin-3-acetic acid (esters, amides) and the products of their chemical transformation – 1H-2-oxo-3-(coumarinyl-3ґ)-4-hydroxyquinolines that had not been investigated before were synthesized.
The new effective method of synthesis of 1H-2-oxo-4-hydroxyquinolin-3-acetic acid was elaborated. It was successfully used in synthesis of в-(1H-2-oxo-4-hydroxyquinolinyl-3)-propionic acid.
Methods for the large-scale preparation of esters and amides of 1H-2-oxo-4-hydroxyquinolin-3-acetic acid from 2,3,4,5-tetrahydrofuro-[3,2-c]-quinolin-2,4-dione were suggested.
The peculiarities of steric structure of dialkylamides of 1H-2-oxo-4-hydroxyquinolin-3-acetic acid were investigated.
As a result, thyroidtropic, anti-inflammatory, diuretic, antibacterial (including antituberculosis) activity of the compounds synthesized was studied.
The most potent anti-inflammatory and antithyroid agents were identified. It is presently undergoing an extensive pharmacological evaluation. Several structure-activity relationships were developed.
Key words: 1H-2-oxo-4-hydroxyquinolin-3-acetic acid, esters, amides, coumarine, synthesis, X-ray assay, anti-inflammatory, antithyroid activity.
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