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Registration Number

0216U006264, 0114U002202 , R & D reports

Title

The calixarenes and azacrown ethers based molecular platforms to create effective antiviral drugs

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Head

Kuzmin Viktor Evgenyevich,

Registration Date

24-02-2016

Organization

A.V.Bogatsky Physico-Chemical Institute of the National Academy of Sciences of Ukraine

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The object of the study: Calix[4]arenes, azacrown-ethers, 6-aminohexanoic and 4-aminomethylbenzoic acids, cytotoxicity, anti-influenza activity. Objective: creation based on molecular platforms Calix[n]arenes and azacrown-ethers, compounds which are capable of display antiviral activity due to the presence in their composition fragments of molecules of known and potential antiviral drugs, and improve the bioavailability of known antivirals as supramolecular ensembles that are able to play the role of transmembrane carriers and hubs (Drug Organizers), and the study of the biological activity of the compounds obtained. By joining macrocyclic molecules of different platforms of several antiviral agents can achieve effects of combining and concentration, which will increase the therapeutic efficacy of combined antiviral drugs. Bottom Line: It is shown that diazacrown-ethers are the most promising molecular platforms (Drug Organizers) to create new effective antiviral agents. Conjugation of esters of drugs such as 6-aminohexanoic and 4-aminomethylbenzoic acids causing a significant increase in activity (lgTID50) against influenza virus H3N2. In particular, the most active is N,N-'bis(6-aminohexanoyl)diaza-18-crown-6. It significantly inhibits virus reproduction (lgTID50 = 3.9) at a concentration of 1.10-3 mol/l in the absence of cytotoxicity. Initial preparations at this concentration is inactive.USES: Bioorganic Chemistry

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І. М. Ракипов
А. Ф. Луцюк
В. Є. Кузьмін
М. К. Кулінський
О. В. Мазепа
О. О. Алєксєєва
С. С. Басок
Т. В. Михайлова
Ю. О.Карнаухова

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2020-04-02