Syumka Y. «Synthesis, chemical and biological properties of mono- and bis-derivatives of spiro-2-oxindole [3,3']pyrrole»

Українська версія

Thesis for the degree of Candidate of Sciences (CSc)

State registration number

0419U002449

Applicant for

Specialization

  • 15.00.02 - Фармацевтична хімія та фармакогнозія

17-05-2019

Specialized Academic Board

Д 64.605.01

National University of Pharmacy

Essay

The thesis is dedicated to the synthesis of the new biologically active compounds among mono- and bis-derivatives of spiro-2-oxindole-[3,3']-pyrrole and study of their pharmacological activity. New hexamethylene(ethylene, oxalyl amine, m-phenylene)-N,N'-bis(spiro-indole-3,3'-pyrrolo[3,4-c]pyrrole-2a,5a'-di-hydro-2,2',6'(1H,1'H,5'H)-triones) and and their monoanalogs were synthesized via 1,3-dipolar cycloaddition of azomethinilides obtained in situ from isatines and α-amino acids with various dipolarophils based on bis-maleimides. The course of this reaction is investigated depending on the relationship and nature of the reagents, the solvent and its mechanism. The possibilities of nitrosation, alkylation and acylation of the obtained substances were investigated. The structure of compounds synthesized was confirmed by IR-, 1H, 13C NMR-spectroscopy, mass-spectrometry and elemental analysis. Found compounds that exhibit pronounced antimicrobial, antioxidant, anti-inflammatory activity and inhibit properties in relation to fibroblasts growth factor receptor (FGFR1) and are promising biologically active substances.

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