Nosulenko I. Synthesis, physico-chemical and biological properties of 2-[(3-R-2-оxo-2Н-[1,2,4]triazino[2,3-c]quinazolin-6-yl)thio]acetic acids and then substituted

Українська версія

Thesis for the degree of Candidate of Sciences (CSc)

State registration number

0415U004902

Applicant for

Specialization

  • 15.00.02 - Фармацевтична хімія та фармакогнозія

23-10-2015

Specialized Academic Board

Д 35.600.02

Danylo Halytsky Lviv National Medical University

Essay

Objects - [5+1]-cyclocondensation processes in synthesis of novel bioactive substituted potassium 2-oxo-2Н-[1,2,4]triazino-[2,3-с]quinaziline-6-thiolates, alkylation, hydrolysis, ammonolysis, neutralization in synthesis of prospective bioactive substituted 2-[(3-R-2-oxo-2H-[1,2,4]triazino[2,3-c]quinazolin-6-yl)thio]acetic acid and their functional derivatives. Aims - elaboration of synthetic methods for substituted potassium 3-R-2-oxo-2Н-[1,2,4]triazino[2,3-с]quinazolin-6-thiolates and 2-[(3-R-2-oxo-2Н-[1,2,4]triazino[2,3-c]quinazolin-6-yl)thio]acetic acids and their derivatives, studying of their physicochemical and biological properties, evaluation of "structure - bioactivity" correlation among synthesized compounds. Methods - experimental methods of organic chemistry: synthesis, physicochemical method of analysis (IR-, 1Н and 13С NMR-spectrometry, chromato-mass and mass-spectrometry), pharmacological screening in vitro and in vivo, QSAR-analysis molecular docking. Results - methodology of formation for combinatorial library of bioactive 2-[(3-R-2-oxo-2Н-[1,2,4]triazino[2,3-c]quinazolin-6-yl)thio]acetic acids amides. Bioactive compounds with actoprotective, cerebroprotective, antimicrobial, antiviral and antitumor activities. Results implemented in studying process. Branch of knowledge - pharmacy.

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