Altuhov O. Synthesis, properties and conversion of а-arilarnido-?-(2-oksoindolinilden-3)-acetic acid

Українська версія

Thesis for the degree of Candidate of Sciences (CSc)

State registration number

0411U006257

Applicant for

Specialization

  • 15.00.02 - Фармацевтична хімія та фармакогнозія

07-10-2011

Specialized Academic Board

Д 64.605.01

National University of Pharmacy

Essay

The target-directed synthesis of the potential nootropic, antihypoxant, antiviral and anabolic agents among the а-arylamido-а-(2-oxoindolinylidene-3)-acetic acids has been carried out. The preparative methods were developed for the synthesis of the new groups of biologically active compounds: (2Z)-(benzoylamino)(1-R-2-oxo-1,2-dihydro-3Н-indol-3-ylidene)acetic acids, its esters, azlactones and amides, N-[2-(benzoylamino)(2-oxo-1,2-dihydro-3Н-indol-3-ylidene)aminoacids and its esters. The structure of the compounds synthesized have been confirmed by the data of the elemental analysis, UV-, IR- and NMR-spectroscopy, their purity and individuality was proved by thin-layer chromatography (TLC). The pharmacological screening showed the number of perspective nootropic, antihypoxant, antiviral and anabolic agents. The most active one - N-{(1Z)-2-oxo-1-(2-oxo-1,2-dihydro-3Н-indol-3-ylidene)-2-[(2-phenilethyl)amino]ethyl} benzamide has been recommended for preclinical biological researches as potential preparation with antihypoxant action.

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