Kiz O. Synthesis, chemical and biological properties of 1-aryl-pyrrolidin-2,4-dion derivatives

Українська версія

Thesis for the degree of Candidate of Sciences (CSc)

State registration number

0410U002585

Applicant for

Specialization

  • 15.00.02 - Фармацевтична хімія та фармакогнозія

28-05-2010

Specialized Academic Board

Д 64.605.01

National University of Pharmacy

Essay

In order to find new biologically active compounds among the derivatives of 1-aryl-pyrrolidin-2,4-dione the methods of synthesis have been investigated and series of 4-hydroxy-l-aryl-l,5-dihydropyrrol-2-on-3-carboxylic acids amides, 4-R-amino-l-aryl-1,5-dihydropyrrol-2-ones, 4-O-alkyl-1-aryl-l,5-dihydropyrrol-2-ones, pyrrolidin-2,4-dion 3-iliden derivatives, 4-hydroxy-1-R-3-(1H-4-benzoimidazol-2-yl)-1,5-dihydropyrrol-2-ones has been synthesized. The tautomerism and reactivity of 4-hydroxy-l-aryl-2-oxo-l,5-dihydropyrrol-3-carboxylic acids ethyl esters and 1-aryl-pyrrolidin-2,4-diones has been studied. The structure and individuality of the obtained compounds have been proved by the methods of NMR-, UV- and IR-spectroscopy, mass-spectrometry, HPLC, TLC, element analysis and by the chemical methods. The pharmacological activity of the new compounds has been investigated. The analgesic, anti-inflammatory, antioxidant, membrane stabilizing properties and antimicrobial activity for these derivatives have been determined.For the further pharmacological study 4-(2-methyl)phenyl-l,5-dihydropyrrol-2-on has been suggested. This substance has the combined analgesic, antiinflammatory, antioxidant, membrane stabilizing properties. The methods of standardization of this compound have been developed

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