Search for antibacterial and antiprotozoal compounds in alkaloid beta-carboline series

УДК 619: 616. 993.192
DOI 10.33861/2071-8020-2023-4-42-44

Zubenko A. A., Fetisov L. N., Svyatogorova A. E., Avagyan E. N., Divaeva L. N.

Summary. An actual direction in the search for drugs is the modifcation of natural compounds with known biological activity. Alkaloids and their derivatives have a considerable potential for transformation into biologically active structures. A signifcant number of modern medicinal substances are based on natural origin. Among natural compounds, alkaloids represent the most interesting class of chemicals. Our research is aimed at creating anti-infective agents of a non-antibiotic nature, which is especially important in connection with the growing problem of drug resistance of microorganisms. Under the conditions of TC «Khim. synthesis» of the North Caucasian Zonal Research Veterinary Institute, a branch of the Federal State Budgetary Scientifc Institution «Federal Rostov Agrarian Research Center», synthesis of compounds of a number of beta-carboline alkaloid derivatives was carried out. The syntheses were carried out using known methods described in manuals on organic chemistry and in the literature. For all compounds, the level of antiprotozoal activity was determined on the model of ciliates of the species Colpoda steinii and indicators of antibacterial activity against grampositive bacteria St. aureus and gram-negative bacteria E. coli. It was found that among the studied alkaloid derivatives, all synthesized compounds were active against protozoa, but the level of their activity was insignifcant. On the contrary, the antibacterial activity of the compounds turned out to be more signifcant. All structures were active against both Gram-positive St. aureus and Gram-negative E. coli bacteria. The level of activity of betacarboline alkaloid derivatives against St. aureus was 70.5% of the activity level of furazolidone and 50% of the activity level of ciprofloxacin; the level of activity against E. coli was 66% of the activity level of furazolidone and 44% of the activity level of ciprofloxacin.

Keywords: synthesis of beta-carboline alkaloid derivatives, screening of antibacterial and antiprotozoal activity, colpods, Escherichia coli, Staphylococcus aureus.

Author affiliation:

Zubenko Aleksandr A., D. Sc. in Biology, chief scientifc researcher of the North Caucasian Zonal Scientifc-Research Veterinary Institute - branch of the Federal Rostov Agrarian Scientifc Center; 0, Rostovskoe hgw., Novocherkassk, Rostov region, 346421; phone: 8-928-6049743; e-mail: alexsandrzubenko@yandex.ru.

Fetisov Leonid N., Ph.D. in Veterinary Medicine, leading scientifc researcher of the North Caucasian Zonal Scientifc-Research Veterinary Institute - branch of the Federal Rostov Agrarian Scientifc Center; 0, Rostovskoe hgw., Novocherkassk, Rostov region, 346421; phone: 8-908-1978224; e-mail: fetisoff.leonid2018@yandex.ru.

Avagyan Elen Nverovna, laboratory researcher of the North Caucasian Zonal Scientifc-Research Veterinary Institute - branch of the Federal Rostov Agrarian Scientifc Center; 0, Rostovskoe hgw., Novocherkassk, Rostov region, 346421; phone: 8-908-1882434; e-mail: elen.avagyan.1999@inbox.ru.

Divaeva Lyudmila N., Ph. D. in Chemistry, leading scientifc researcher of the Laboratory of Organic Synthesis of the Research Institute of Physical and Chemical Chemistry of the Southern Federal University; 194/2, Stachki av., Rostov-on-Don, 344090; phone: 8-928-1756654; e-mail: divaevaln@mail.ru.

Responsible for correspondence with the editorial board: Svyatogorova Aleksandra E., junior scientific researcher of the North Caucasian Zonal Scientific-Research Veterinary Institute — branch of the Federal Rostov Agrarian Scientific Center; 0, Rostovskoe hgw., Novocherkassk, Rostov region, 346421; phone: 8-988-9525755; e-mail: sviatogorova.a@yandex.ru.