Rizak G. Synthesis, physical, chemical and biological properties of 2-,4-dioxo- and 4-imino-20oxo-3phenyl-5-R-6-R'-thieno[2,3-d]pyrimidines

Українська версія

Thesis for the degree of Candidate of Sciences (CSc)

State registration number

0412U005134

Applicant for

Specialization

  • 15.00.02 - Фармацевтична хімія та фармакогнозія

31-05-2012

Specialized Academic Board

Д 64.605.01

National University of Pharmacy

Essay

The features of interactions of 2-amino-3-carbethoxy(cyano)thiophenes with phenylisocyanate were studied and the cyclization processes of their derivatives formed into the corresponding 2,4-dioxo- and 4-imino-2-oxo-3-phenyl-5-R-6-R'-thieno[2,3-d]pyrimidines were also studied. The characteristics of alkylation and acylation of thieno[2,3-d]pyrimidines synthezed were examined. It was found that the reactions take place on exocyclic Oxygen with the formation of 2-alkyl(acyl)oxiderivatives. When thieno[2,3-d]pyrimidines are treated with acrylonitrile 3-(2,4-dioxo-3-phenyl-5-R-6-R'-thieno[2,3-d]pyrimidin-1-yl) nitriles of propanoic acids are formed; acidic hydrolysis of which leads to the corresponding propanoic acids; with hydroxylamine - corresponding amidoximes. On the virtual screening (the program PASS) data diuretic, anti-inflammatory and antimicrobial action of the synthesized compounds was carried out. Some conformities "structure-action" were established.

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