14 research outputs found
Synthesis of new derivants 11h-indeno[1,2-b] - quinoxaline as perspective inhibitors of JNK (C-Jun n-terminalnal kinase)
Various quinoxalines show biological activity and have such properties as antiviral, antibacterial, antimicrobial, anti-inflammatory, anticancer, antidepressant, vermicidal, and act as inhibitors of kinases [1]. JNK family enzymes (C-Jun N-terminal kinase) are involved in an embryonal heart development, a regulation of metabolism and normal functioning of a myocardium. Besides, they play an important role in the signaling pathways which lead to apoptosis and necrosis and, also, they regulate processes by which damage of brain neurons and cardiomyocytes during ischemia are depended on. In this regard, the development of specific inhibitors of JNK is a relevant objective of medical chemistry. Derivants with 11H-indeno[1,2-b]-quinoxaline system are described in literature, but there is not a lot of them. For example, it is known only 45 replaced (generally - methyl, nitro - alkoxy-, carboxyl groups) 11Hindeno[1,2-b]- quinoxaline-11-ones according to Reaxys base. For some of them provided data about inhibition of enzymes (glucosidase, SYK kinase) anticarcinogenic activity. Someone systematic researches on influence of the nature of the substituting group on activity and bioavailability of 11H-indeno [1,2-b]- quinoxalines are still unknown of carrying out. The expected results are urgent to from the fundamental and practical point of view. Methods of synthesis of new derivants of 11H-indeno[1,2-b] -quinoxaline will be developed, which will make a contribution to chemistry of the condensed heterocyclic systems. The obtained data will make a contribution to rational design of medicines for treatment of these diseases. Existence in synthesizable molecules of ionizable and biocompatible group does them by potentially more bioavailable and will give an opportunity for creation on their basis of pharmaceuticals
ΠΡΡΠ»Π΅Π΄ΠΎΠ²Π°Π½ΠΈΠ΅ ΠΊΠΎΡΡΠΎΠ·ΠΈΠΎΠ½Π½ΡΡ ΡΠ²ΠΎΠΉΡΡΠ² Π±ΠΈΠΎΡΠΎΠ²ΠΌΠ΅ΡΡΠΈΠΌΡΡ ΠΏΠΎΠΊΡΡΡΠΈΠΉ Π½Π° ΠΎΡΠ½ΠΎΠ²Π΅ ΡΠΈΡΠ°Π½Π°, ΠΎΡΠ°ΠΆΠ΄Π΅Π½Π½ΡΡ ΠΌΠ΅ΡΠΎΠ΄ΠΎΠΌ ΡΠ΅Π°ΠΊΡΠΈΠ²Π½ΠΎΠ³ΠΎ ΠΌΠ°Π³Π½Π΅ΡΡΠΎΠ½Π½ΠΎΠ³ΠΎ ΡΠ°ΡΠΏΡΠ»Π΅Π½ΠΈΡ
Π ΡΠ°Π±ΠΎΡΠ΅ ΠΈΠ·ΡΡΠ°Π»ΠΈΡΡ ΡΠ²ΠΎΠΉΡΡΠ²Π° Ti-O-N ΠΏΠΎΠΊΡΡΡΠΈΠΉ, Π½Π°Π½Π΅ΡΠ΅Π½Π½ΡΡ
Π½Π° ΡΡΠ°Π»ΡΠ½ΡΠ΅ ΠΏΠΎΠ΄Π»ΠΎΠΆΠΊΠΈ ΠΌΠ΅ΡΠΎΠ΄ΠΎΠΌ ΡΠ΅Π°ΠΊΡΠΈΠ²Π½ΠΎΠ³ΠΎ ΠΌΠ°Π³Π½Π΅ΡΡΠΎΠ½Π½ΠΎΠ³ΠΎ Π½Π°ΠΏΡΠ»Π΅Π½ΠΈΡ, ΡΠ°ΠΊΠΈΠ΅ ΠΊΠ°ΠΊ ΠΊΠΎΡΡΠΎΠ·ΠΈΠΎΠ½Π½Π°Ρ ΡΡΠΎΠΉΠΊΠΎΡΡΡ, ΡΠ΅ΡΠΌΠΈΡΠ΅ΡΠΊΠ°Ρ ΡΡΡΠΎΠΉΡΠΈΠ²ΠΎΡΡΡ, Π° ΡΠ°ΠΊ ΠΆΠ΅ Π΄ΠΈΡΡΡΠ·ΠΈΠΎΠ½Π½ΡΠ΅ ΠΏΡΠΎΡΠ΅ΡΡΡ Π² ΡΠΈΠ·ΠΈΠΎΠ»ΠΎΠ³ΠΈΡΠ΅ΡΠΊΠΈΡ
ΡΠ°ΡΡΠ²ΠΎΡΠ°Ρ
. ΠΠ΅ΡΠΎΠ΄Π°ΠΌΠΈ ΠΈΠ½ΡΡΠ°ΠΊΡΠ°ΡΠ½ΠΎΠΉ ΡΠΏΠ΅ΠΊΡΡΠΎΡΠΊΠΎΠΏΠΈΠΈ ΠΈ Π°ΡΠΎΠΌΠ½ΠΎ-ΡΠΌΠΈΡΡΠΈΠΎΠ½Π½ΠΎΠ³ΠΎ Π°Π½Π°Π»ΠΈΠ·Π° Π±ΡΠ»Π° ΡΡΡΠ°Π½ΠΎΠ²Π»Π΅Π½Π° Ρ
ΠΈΠΌΠΈΡΠ΅ΡΠΊΠ°Ρ ΠΈΠ½Π΅ΡΡΠ½ΠΎΡΡΡ ΠΏΠ»Π΅Π½ΠΊΠΈ, Π° ΡΠ°ΠΊ ΠΆΠ΅ ΠΏΠΎΡΠ΅Π½ΡΠΈΠ°Π»ΡΠ½Π°Ρ Π±ΠΈΠΎΠ»ΠΎΠ³ΠΈΡΠ΅ΡΠΊΠ°Ρ Π°ΠΊΡΠΈΠ²Π½ΠΎΡΡΡ Π² Π²ΠΈΠ΄Ρ ΠΎΠ±Π½Π°ΡΡΠΆΠ΅Π½ΠΈΡ ΠΎΠΊΡΠΈΠ΄Π° Π°Π·ΠΎΡΠ° Π² ΠΌΠΎΠ΄Π΅Π»ΡΠ½ΡΡ
ΡΠ°ΡΡΠ²ΠΎΡΠ°Ρ
ΠΏΠΎΡΠ»Π΅ ΠΊΠΎΠ½ΡΠ°ΠΊΡΠ° Ρ ΠΏΠΎΠΊΡΡΡΠΈΡΠΌΠΈ Ti-O-N.The properties of Ti-O-N coatings deposited on steel substrates by the method of reactive magnetron sputtering, such as corrosion resistance, thermal stability, as well as diffusion processes in physiological solutions were studied. By the methods of infrared spectroscopy and atomic emission analysis, the chemical inertness of the film was established, as well as the potential biological activity in the form of detection of nitrogen oxide in model solutions after contact with Ti-O-N coatings