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Registration Number

0215U000439, 0113U003187 , R & D reports

Title

Development of the theoretical basis for the synthesis of new nitrogen- and sulfur-containing compounds - potential drug substances with various biological actions.

Head

V. Novikov,

Registration Date

24-02-2015

Organization

Lviv Polytechnic National University

Description

The methods of synthesis of new thiosulfonate, sulfide and heterocyclic derivatives, new aminoacid derivatives of naphthoquinone with phenol screened moiety were developed and ways of possible practical applications were investigated. By selective introduction of pharmacophore fragments as substituents in the core of heterocycle, a convenient preparative methods of obtaining new quinazolines, phenothiazines, pyrimidines were developed and their physical and chemical properties were investigated. Different ways of thiosulfonate introduction in quinazoline structure were explored. Interaction of 4-chloroquinazoline with alkyl S-esters of 4-aminobenzen-thiosulfoacid with obtaining thiosulfonate derivatives was explored. On the basis of the received results preparative methods of obtaining thiosulfoacid esters of quinazoline were investigated. New sulfuro- and nitrogen-containing phenothiazine derivatives - disulfide, thiol, sulfide, thiosulfonate based on phenothiazine and 2- chlorophenothiazine were obtained. Based on synthesized thiosemicarbazone phenothiazine derivatives cyclization reaction with forming thiazoline derivatives of phenothiazine was carried out. Methods of obtaining acyl-isothiocyanates from synthesized aminoacid derivatives of 2,3-dichloro-1,4-naphthoquinone were developed and the their physical and chemical properties were studied. New potentially biologically active compounds were obtained by reacting of 3-chloro-2-(3,5-di-tert-butyl-4-hydroxyphenyl)-1,4-naphthoquinone with secondary and primary amines and also aminoacids. Physicochemical properties of the synthesized derivatives of quinoxaline, phenothiazine, naphthoquinone, pyrimidine were studied. A computer screening of predicted biological activity by program PASS for synthesized compounds was carried out and compounds with the highest rates of different types of activity (bactericidal, fungicidal, anticancer, etc.) were isolated. By experimental biological studies high antibacterial and fungicidal activity of some synthesized compounds were revealed. Results of the study on the influence of membrane-bound tyrosine kinase identified compounds that are inhibitors of tyrosine kinases.5481

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Болібрух Х.Б.
Василюк С.В.
Карпенко О.Я.
Кархут А.І.
Ковальчук О.І.
Крвавич А.С.
Литвин Б.Я.
Лубенець В.І.
Монька Н.Я.
Новіков В.П.
Фігурка О.М.
Хом'як С.В.
Хоміцька Г.М.
Шиян Г.Б.
Яремкевич О.С.