MOSCOW, Oct. 25Russian scientists have identified new candidate molecules for the treatment of tuberculosis. At the Ural Federal University named after the first President of Russia B.N. Yeltsin (Ural Federal University) obtained coumarin derivatives and proved the effectiveness of their effect on the infectious disease caused by the Koch bacillus. In addition, the researchers say that the resulting compounds may also affect a wider range of infections that are resistant to existing antibiotics. The results are presented in Pharmaceuticals.
Today, medicine knows more than a thousand different infectious diseases; the method of their treatment depends on the nature of the pathogen. Despite the large range of medications that effectively deal with viruses and pathogenic microorganisms, humanity needs to constantly increase its arsenal of means to combat them. This is due to the acquisition of resistance to existing drugs. Therefore, scientists around the world are in search of new substances with proven biological activity.
One of these substances, according to scientists from the Ural Federal University named after the first President of Russia B.N. Yeltsin (Ural Federal University), these are coumarins. Coumarin and its derivatives are found in many plants, mainly in the form of glycosides. When plants dry out, the smell of fresh hay appears as a result of the breakdown of glycosides. Coumarin is used in the preparation of perfume compositions, fragrances for cosmetic products and tobacco flavoring.
As Grigory Zyryanov, chief researcher at the laboratory of advanced materials, green methods and biotechnologies of UrFU, said, this class of compounds has a huge medicinal value potential.
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“We have been working with coumarins for a long time, using them as fluorescent dyes and dyes for bioimaging,” he noted, emphasizing that coumarins are part of many drugs — antibiotics, analgesics, antitumor and antiviral drugs.
In addition, according to the scientist, coumarins are easily synthesized and modified, and their derivatives are guaranteed to have biological activity. “They are traditionally found in many natural compounds, that is, they are focused on green chemistry,” emphasized Grigory Zyryanov.
In vitro experiments were carried out by Russian scientists in collaboration with Indian colleagues. Researchers have synthesized new compounds — 4-methyl-7-substituted coumarins.
“Using computer power, we previously established what chemical formulas substances with guaranteed antiviral activity based on coumarins and triazole (a key component of many medications) should have. Then we synthesized 55 substances, 4 of which showed high activity against tuberculosis pathogens,” — noted Zyryanov. According to scientists, this is especially important against the backdrop of the emergence of resistant tuberculosis, which cannot be treated with existing drugs on the market.
In the future, UrFU employees plan to evaluate the toxicity of selected promising candidates and “move towards experiments on animals» with subsequent entry into clinical trials.
Ural Federal University is a participant in the state support program for universities of the Russian Federation «Priority-2030» of the national project «Science and Universities».