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Information × Registration Number 0215U004237, 0112U001742 , R & D reports Title Structural patterns of functioning of novel hetero- and macroheterocycles as potential biologically active compounds popup.stage_title Head Galkin Boris Mikolayovich, Registration Date 17-02-2015 Organization Odesa I.I.Mechnikov national university.Pervomaisk institute. popup.description2 The objects of investigations - the derivatives of dihydro- and tetrahydropyrimidine, the synthetic porphyrins with heterocyclic meso-substituents quaternized by halogen- and tosyloxyalkylsulfonic acids with different alkyl chain length. The goal of the work - to establish of the concept of targeted search for effective and safe nootropics and actoprotectors based on the study of pharmacological activity, depending on the structure of pyrimidine derivatives and decisive influence of the nature of zwitterionic substituents on the behavior of porphyrin compounds in biological systems. The main hypothesis of the project - knowledge of the mechanisms of action of substances that have nootropic and actoprotective activity, as well as the relationship between their structure and biological activity can serve as a basis for the purposeful creation of highly effective and safe and nootropics and actoprotectors. Antimicrobial activity of porphyrins is largely determined by the nature zwitterionic substituents in the macrocycle. А potential actoprotectors and antihypoxants have been synthesized based on 4,5-substituted pyrimidines, thiopyrimidine, 5-alkyl-2-thiobarbituric acid, quinazolinethiones and 1,4-benzodiazepin-2-thiones with aminoalkyl and arylpiperazinylbutyl substituents. Their pharmacological activity were studied in models of normobaric hypoxia, hemic hypoxia, normothermia, hypothermia and hyperthermia. It is shown that derivatives of 2-mercaptopyrimidine have expressed actoprotective and antihypoxic activity, stimulate high performance under extreme loads and to exceed the reference drug activity bemithyl. These compounds also have high anxiolytic activity. All of the above mentioned makes these materials very attractive as potential drugs - actoprotector, antihypoxants and anxiolytics. Zwitterionic porphyrins isomeric quinolinyl substituents, quaternized difunctional quaternizing agents showed significant antimicrobial activity against the test strains of pathogenic microorganisms suspended in moderate toxicity to the cell cultures. Product Description popup.authors Ішков Юрій Васильович Водзінський Сергій Валентинович Ганевич Віктор Миколайович Кириченко Ганна Михайлівна Соболєва Світлана Григорівна popup.nrat_date 2020-04-02 Close