2023-05-18 14:22:00
Therefore, researchers continue to actively search for new drugs. In a new work, Russian scientists from the Federal Research Center for Biotechnology of the Russian Academy of Sciences, in collaboration with colleagues from the United States and Italy, made a successful attempt to obtain a prototype drug that would be able to kill the human immunodeficiency virus in its “den”, in neurons. Thus, for the first time, the combined international team came closer to obtaining a cure for HIV, rather than making the disease chronic.
To do this, they modeled, synthesized, optimized and studied in detail the biological activity of more than 250 original compounds derived from N-phenyl-1-(phenylsulfonyl)-1H-1,2,4-triazole-3-amines. The initial idea was to create a new generation of drugs – inhibitors of HIV reverse transcriptase (the enzyme responsible for the “reproduction” of the virus), while such drugs should successfully pass through the blood-brain barrier, penetrate into neurons, destroy the virus there and be non-toxic to the nerve cells themselves. The latter, the researchers told us, proved to be the most difficult: it was necessary to create a drug that was effective enough at a concentration that did not harm the cells of the host organism.
To understand how this class of drugs works, let’s briefly explain how viruses reproduce themselves. RNA viruses, including HIV, need to translate their hereditary information from RNA into DNA. This is necessary to force the cell to synthesize new virus particles, because viruses cannot reproduce without using the hereditary mechanism of the host cells. To suppress the work of the viral enzyme, scientists have proposed a new generation of non-nucleoside HIV reverse transcriptase inhibitors that block the active center of the virus enzyme. Invented molecules prevent the enzyme from changing shape, which is necessary for its normal operation. As a result, the virus cannot replicate copies of itself that could infect new cells. About the results of their work, scientists told in the world’s leading journal in the field of new drug development, the Journal of Medicinal Chemistry.
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