Isayev S. Synthesis, reactionary ability and biological activity derivatives o-halogenbenzoic, aromatic aminoacides and acridine.

Українська версія

Thesis for the degree of Doctor of Science (DSc)

State registration number

0509U000136

Applicant for

Specialization

  • 15.00.02 - Фармацевтична хімія та фармакогнозія

23-01-2009

Specialized Academic Board

Д64.605.01

Essay

The thesis is devoted to the development of new promising scientific approach in the synthesis of BAS on the basis of o-halogenbenzoics, aromatic and acridine. On the basis of methods developed there has been out the synthesis of about 900 new substances (Pat. №33114A, inform. letters №118-98, 43-03, 266-03, 45-07). By means of modern physico-chemical methods their structure and reaction ability have been determined. The constants of ionization N-phenylanthranilic acids (N-PhAA) and factors of their distribution in water-octanole of a mix. The technique of quantivative definition N-PhAA substituente by a method of biphase titration in system octanol-water is offered. The kinetics of the alkaline hydrolysis reaction for methyl esters of 3-nitro-N-PhAA in binary dioxin-water were studied in temperature 318-358K. The acid-base properties for properties for substituents of 9-chlor-, 9-hydrazinoacridine, 9-thioacridone were investigated. There has been carried out the pharmacological screening of the synthesized throung 24 testes. For the most perspective substance - ethyl ester 4-carbethoksioxamoilhydrazid oxanilic acid (benodiox) - preclinical investigation were carried out. Experimental and industrial synthesis development of benzodiox and methods of standartization

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