NEW C1 AND N5 DERIVATIVES OF CERPEGINE. SYNTHESIS AND ANTIBACTERIAL ACTIVITY STUDY

This study explores the bioactive properties of synthetic compounds containing γ-lactone and 2-pyridone ring systems, which exhibit a broad spectrum of pharmacological activities. These compounds are structural analogues of the alkaloid serpegin, originally isolated from Ceropegia juncea, a plant known in traditional Indian medicine for its therapeutic effects. Serpegin has been reported to possess sedative, anti-inflammatory, analgesic, and anti-ulcer properties, making its synthetic analogues attractive candidates for the development of novel therapeutic agents. Among the synthetic derivatives discussed in this work are compounds C1 and N5, which have demonstrated the ability to enhance cellular responses to interferons and selectively inhibit the activity of the mammalian 20S proteasome. These biological effects suggest that such derivatives may have potential applications in the treatment of immune-related and proliferative disorders, with the added benefit of potentially reduced side effects compared to existing drugs. The antibacterial activity of 37 newly synthesized serpegin derivatives was evaluated using the agar diffusion method under aseptic conditions, with a bacterial load of 20 million microbial cells per milliliter. Both Gram-positive and Gram-negative reference bacterial strains were tested. The results revealed that compounds from the first group exhibited noticeable antibacterial effects, especially against Shigella flexneri, with several compounds showing moderate activity. These findings underscore the significance of further research into the antibacterial properties of serpegin-based compounds, particularly against a wider spectrum of Gram-negative bacteria. This could ultimately contribute to the development of new and effective antibacterial agents with improved selectivity and safety profiles. For citation: Hakobyan R.M., Adunts H.V., Attaryan H.S., Muradyan R.E., Arakelyan H.G., Mirakyan N.A., Davinyan A.M., Mamyan S.S., Melikyan G.S. New C1 and N5 derivatives of cerpegine. synthesis and antibacterial activity study. ChemChemTech [Izv. Vyssh. Uchebn. Zaved. Khim. Khim. Tekhnol.]. 2025. V. 68. N 7. P. 35-47. DOI: 10.6060/ivkkt.20256807.7224.