ÓÄÊ 576.89
DOI 10.33861/2071-8020-2025-1-28-31
Original Empirical Research
Zubenko A.A., Fetisov L.N., Svyatogorova A.E., Chekrysheva V.V., Klimenko A.I.
Annotation. Ten new compounds of a number of triazolophthalazines have been obtained by the interaction of the corresponding chlorophthalazines with acid gyrazides. As a result of testing the biological activity of the synthesized compounds, it was found that the substances showed the highest activity against the ciliated protozoa of the species Colpoda steinii. Structure No. 7, having substituents in the form of a methyl group (R) and a 2-hydroxy-5-chlorophenyl derivative (R1), is active at a concentration of 0.975 mcg/ml, which exceeds the activity of the antiprotozoal preparation chloroquine by 8 times. It should be noted that the widely used drug tolrazuril, used in veterinary practice for the treatment of coccidiosis, is active at a concentration of 62 mcg/ml (literature data). Replacing a bromine atom with a chlorine atom with the same other substituents (compound №5) leads to a sharp drop in activity to 250 mcg/ml. Compounds №2, №6 and №10 are comparable in activity to the control drug chloroquine. With this sample (10 structures), it is not possible to draw a conclusion about the effect of certain substituents on antiprotozoal activity, taking into account their volume and donor-acceptor properties. Attention is drawn to the fact that all the presented compounds have pronounced antibacterial activity, and compounds №2 and №5 are not inferior in activity to the drug of the nitrofuran series furazolidone. It seems promising to search for highly effective antibacterial structures in the series of [1,2,4]triazolo[3,4-a]phthalazines. Of all the substances presented, only three of them (№1, №7 and №8) showed weak activity, while significantly inferior to fundazole.
Keywords: triazolophthalazine series compounds, antibacterial activity, antiprotozoal activity, fungistatic activity.
Author affiliation:
Zubenko Aleksandr A., D. Sc. in Biology, Chief Scientific Researcher of the Creative Team for the Chemical Synthesis of New Medicinal Compounds of the North Caucasus Zonal Scientific Research Veterinary Institute – branch of the Federal Rostov Agrarian Scientific Center; 0, Rostov hgw., Novocherkassk, Rostov region, 346421; phone: 8-928-6049743; e-mail: alexsandrzubenko@yandex.ru.
Fetisov Leonid N., Ph. D. in Veterinary Medicine, Leading Scientific Researcher of the Creative Team for the Chemical Synthesis of New Medicinal Compounds of the North Caucasus Zonal Scientific Research Veterinary Institute – branch of the Federal Rostov Agrarian Scientific Center; 0, Rostov hgw., Novocherkassk, Rostov region, 346421; phone: 8-908-1978224; e-mail: fetisoff.leonid2018@yandex.ru.
Chekrysheva Viktoriya V., D. Sc. in Veterinary Medicine, docent, Director of the North Caucasus Zonal Scientific Research Veterinary Institute – branch of the Federal Rostov Agrarian Scientific Center; 0, Rostov hgw., Novocherkassk, Rostov region, 346421; phone: 8-908-5110139; e-mail: veterinar1987@mail.ru Klimenko Aleksandr I., D. Sc. in Agriculture, Academician of the Russian Academy of Sciences, professor, director of the Federal Rostov Agrarian Scientific Center; 1, Institutskaya st. Rassvet sttl., Aksayskiy district, Rostov region, 346735; e-mail: dzni@mail.ru.
Responsible for correspondence with the editorial board: Svyatogorova Aleksandra E., Ph. D. in Agriculture, Scientific Researcher of the Creative Team for the Chemical Synthesis of New Medicinal Compounds, Academic Secretary of the North Caucasus Zonal Scientific Research Veterinary Institute – branch of the Federal Rostov Agrarian Scientific Center; 0, Rostov hgw., Novocherkassk, Rostov region, 346421; phone: 8-988-9525755; e-mail: sviatogorova.a@yandex.ru.
Conflict of Interest Statement: the authors declare no conflict of interest.
http://vetkuban.com/en/num1_202508.html