The basis for drugs suppressing viruses and fungi was created in Zelinsky Institute

Despite the successful use of antibiotics and antifungal drugs in modern medicine, rising resistance to them has been increasingly observed in recent years. In this regard, there is a real need for innovative solutions aimed at stopping this problem and reducing the burden of infection resistant to existing drugs.

In search of a solution to the problem of creating new antifungal and antibacterial agents, the researchers from laboratory № 31 of Zelinsky Institute of Organic Chemistry and the joint laboratory of ZIOC and SUSU (principal investigator – Dr. L. S. Konstantinova) in cooperation with a number of foreign organizations (USA, Switzerland, Germany, Finland) studied previously unknown heterocyclic azoles — 1,2,3-thiaselenazoles. The fundamental basis of this approach was the reaction of the replacement of a sulfur atom by a selenium atom in sulfur-containing heterocycles discovered at ZIOC, which allowed the authors to obtain a number of new classes of compounds containing interconnected sulfur and selenium atoms in the cycle. Among 1,2,3-thiaselenazoles synthesized for the first time, some of them possessed high submicromolar activity and had low toxicity, which emphasizes the value of such approach for a series of multi-resistant pathogens. Using the methods of molecular modeling and quantum mechanics, the mechanism of their biological action, based on the similar activity of sulfur-containing heterocycles, was proposed. It was shown that the higher strength of the sulfur-sulfur bond in 1,2,3-dithiazoles in comparison with the sulfur-selenium bond in 1,2,3-thiaselenazoles was the key reason for a decrease in the energy of the transition state and a simultaneous decrease in the nonspecific toxicity of the latter.

Source:

Tuomo Laitinen, Ilia V. Baranovsky, Lidia S. Konstantinova, Antti Poso, Oleg A. Rakitin, Christopher R. M. Asquith Antimicrobial and antifungal activity of rare substituted 1,2,3-thiaselenazoles and corresponding matched pair 1,2,3-dithiazoles Antibiotics, 2020, 9, 369. DOI: 10.3390/antibiotics9070369.