Scientists Created a New Substance for a Drug Against Tuberculosis

12:40, May 30, 2024

The obtained compounds are not inferior in efficiency to known analogs

New chemical compounds synthesized by Ural scientists and colleagues from India have high anti-tuberculosis activity. The drug was tested in vitro and found to be comparable to Isoniazid and Rifampicin: widely used drugs against tuberculosis. As the scientists explain, it is crucial to create new medications against known diseases, because the causative agents of many infectious diseases acquire resistance to those currently used for treatment. The scientists published detailed information about the new compounds and how to obtain them in the journal Pharmaceuticals. The Russian Science Foundation (grant No. 24-23-00516) and the Russian Ministry of Science and Higher Education (agreement No. 075-15-2022-1118) supported the research.

To obtain new compounds, scientists synthesized several triazolopyrimidines. These compounds share a similar structure with several anti-TB drugs, including Isoniazid.

"We synthesized 21 chemical compounds and found that some have antituberculosis and anti-inflammatory activities comparable to other drugs. Compared with the well-known anti-TB drug Isoniazid, two of our compounds showed comparable activity at lower concentrations of active ingredient: 0.625 µg/mL versus 0.7 µg/mL for Isoniazid and 0.5 µg/mL for Rifampicin. Two other compounds also showed higher anti-inflammatory activity compared to the common anti-inflammatory drug Diclofenac. The inhibitory (suppressive) activity of our compounds amounted to 44% compared to 41% for Diclofenac at a concentration of the active ingredient of 100 µg/mL," explains Grigory Zyryanov, Professor of the Department of Organic and Biomolecular Chemistry at UrFU.

The World Health Organization states that 10.6 million people worldwide were infected with TB in 2021. India accounted for 28% of all TB cases, while 9.2% of patients lived in China, 7% in the Philippines, 5.8% in Pakistan, 4.4% in Nigeria, 3.6% in Bangladesh and 2.9% in the Democratic Republic of Congo. HIV-positive people, those who have diabetes mellitus, and smokers are the most likely to get TB.

"Mycobacterium tuberculosis bacterium causes tuberculosis and most commonly affects the lungs, although it can also affect other organs. The main symptoms of this disease are chest pain when breathing or coughing, fatigue, weight loss, fever, and others. Tuberculosis is quite difficult to treat, and existing drugs can be very toxic, including hepatotoxic, that is, they harm a liver. Therefore, the challenge today is to develop such compounds that would have relatively low toxicity, but at the same time have comparable or higher efficacy than existing drugs," explains Grigory Zyryanov.

According to the researchers, the compounds obtained have the potential to create a drug against tuberculosis with higher efficacy. In the future, the scientists will conduct additional experiments to clarify the level of toxicity of the compounds.

It should be noted that specialists from the Ural Federal University, I. Y. Postovsky Institute of Organic Synthesis, Kuvempu University (India), Smt. Indira Gandhi Government First Grade Women’s College (India), Vignan’s Foundation for Science, Technology and Research (India), and Sri Siddhartha Academy of Higher Education (India) took part in the study.

Reference

According to Rosstat, in 2000, the incidence of tuberculosis in Russia was 90.7 per 100,000 people which is the highest rate in the history of observation. Then, with the improvement of the health care system and early diagnosis of the disease, the rate of this infection decreased: to 30.71 per 100 thousand people in 2021. Nevertheless, Rospotrebnadzor traced a trend of increasing incidence: in 2022, the number of those who fell ill was 31.11 per 100 thousand people.

Sergei Lukyanchenko

The news article was translated by UrFU International Marketing Office.
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