Rusanova S. Synthesis and study of transformation ways of 2-iminocoumarin-3-carboxamides for searching new biologically active substances

Українська версія

Thesis for the degree of Candidate of Sciences (CSc)

State registration number

0405U000715

Thesis Registration Form

0405U000715.pdf

Applicant for

Specialization

  • 15.00.02 - Фармацевтична хімія та фармакогнозія

25-02-2005

Specialized Academic Board

Д64.605.01

Essay

It has been found that reactions of 2-iminocoumarin-3-carboxamides with aryl- or alkylamines, Gewald amines, hydroxylamine and arylhydrazines lead to corresponding iminoderivative. But 2-iminocoumarin-3-carboxamides react with 2-amino-benzophenones by recyclization mechanism and gave corresponding 3-(4-arylquinazolin-2-yl)coumarines. It has been shown that due to strong intramolecular hydrogen bond 2-(N-aryl)iminocoumarin-3-carboxamides easily acetylated by acetic anhydride produce stable N3-acetyl-2-(N-aryl)iminocoumarin-3-carboxamides. The combinatorial libraries of 2-(N-aryl)iminocoumarin-3-carboxamides and N3-acetyl-2-(N-aryl)iminocoumarin-3-carboxamides have been planned, procedures of synthesis of these libraries have been developed and synthesis has been carried out with good effectivity. Possible biological activity of 2-(N-aryl)iminocoumarin-3-carboxamides has been predicted by PASS software. The pharmacological screening of synthesized compounds showed that 2-[N-(4-aminocarbonylphenyl)]iminocoumarin-3-carboxamide is relatively non-toxic and possess high level of hepatoprotector, analgesic and antiexudative action.

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Files

Дисертація Русанової С.В..doc

Додатки к дисертації Русанова С.В-Д О Д А Т К И (титул).doc

Додатки к дисертації Русанова С.В-ДОДАТОК А ( РСА)-16.02.05..doc

Додатки к дисертації Русанова С.В-ДОДАТОК Д-1 (розробка АНД)-16.02.05..doc

Додатки к дисертації Русанова С.В-ДОДАТОК Д-2 (проект АНД RuSV)-16.02.05..doc

Додатки к дисертації Русанова С.В-Таблиця Б.1. (N-Aryl).doc

Додатки к дисертації Русанова С.В-Таблиця Б.2. ПМР (N-Aryl).doc

Додатки к дисертації Русанова С.В-Таблиця Б.3 (acetyl N-aryl).doc

Додатки к дисертації Русанова С.В-Таблиця Б.4. ПМР (acetyl N-aryl).doc

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