vestichИзвестия Национальной академии наук Беларуси. Серия химических наукProceedings of the National Academy of Sciences of Belarus, Chemical Series1561-83312524-2342The Republican Unitary Enterprise Publishing House "Belaruskaya Navuka"10.29235/1561-8331-2021-57-4-431-437vestich-687Research ArticleОРГАНИЧЕСКАЯ ХИМИЯORGANIC CHEMISTRYСинтез пиримидиновых производных на основе халконов и их противомикробная активностьSynthesis of chalcone-based pyrimidine derivatives and their antimicrobial activityМартинкевичД. С.MartsinkevichD. S.

Мартинкевич Денис Сергеевич – мл. науч. сотрудник

ул. Ф. Скорины, 36, 220141, Минск, Республика Беларусь

Denis S. Martsinkevich – Junior Researcher

36, F. Skaryna str., 220141, Minsk, Republic of Belarus

den13martinkevich@gmail.comЧернявскаяЕ. Ф.ChernyavskayaK. F.

Чернявская Екатерина Федоровна – ассистент кафедры биотехнологии

ул. Свердлова, 13 а, 220006, Минск, Республика Беларусь

Katerina F. Chernyavskaya – Assistant of Biotechnology Department

13 a, Sverdlova str., 220006, Minsk, Republic of Belarus

chernyavskaya@belstu.byТарасевичВ. А.TarasevichV. A.

Тарасевич Владимир Александрович – д-р хим. наук, профессор, гл. науч. сотрудник

ул. Ф. Скорины, 36, 220141, Минск, Республика Беларусь

Vladimir A. Tarasevich – D. Sc. (Chemistry), Professor, Chief Researcher

36, F. Skaryna str., 220141, Minsk, Republic of Belarus

tar@ichnm.byИнститут химии новых материалов НАН БеларусиInstitute of Chemistry of New Materials of the National Academy of Sciences of BelarusБелорусский государственный технологический университетBelarusian State Technological University202103122021574431437Copyright © Мартинкевич Д.С., Чернявская Е.Ф., Тарасевич В.А., 20212021Мартинкевич Д.С., Чернявская Е.Ф., Тарасевич В.А.Martsinkevich D.S., Chernyavskaya K.F., Tarasevich V.A.Данная работа распространяется под лицензией Creative Commons Attribution 4.0.This work is licensed under a Creative Commons Attribution 4.0 License.https://vestichem.belnauka.by/jour/article/view/687

Синтезирован ряд замещенных халконов и пиримидиновых производных на их основе. Исследована противомикробная активность полученных соединений, а также их способность усиливать действие существующих противомикробных средств. Синтезированные на основе халконов пиримидиновые производные обладают антибактериальной и противомикробной активностью, а также способны усиливать противомикробную активность существующих препаратов.

A series of substituted chalcones and pyrimidine derivatives on their base was synthesized. Obtained compounds were tested for antimicrobial activity and ability to increase activity of known antimicrobial substances. Pyrimidine products shown good activity against Staphylococcus aureus and Candida tropicalis. These compounds also could increase activity of modified polyguanidines against Staphylococcus aureus.

халконыгуанидинциклоконденсацияпиримидиныпротивомикробная активностьchalconesguanidinecyclocondensationpyrimidinesantimicrobial activityReferencesRecent developments in biological aspects of chalcones: the odyssey continues / A. Rani [et al.] // Expert Opinion on Drug Discovery. – 2019. – Vol. 14, N 3. – P. 249–288. https://doi.org/10.1080/17460441.2019.1573812Rani A., Anand A., Kumar K., Kumar V. Recent developments in biological aspects of chalcones: the odyssey continues. Expert Opinion on Drug Discovery, 2019, vol. 14, no. 3, pp. 249–288. https://doi.org/10.1080/17460441.2019.1573812Chalcone synthesis, properties and medicinal applications: a review / A. Rammohan [et al.] // Environ Chem Lett. – 2020. – Vol. 18, N 2. – P. 433–458. https://doi.org/10.1007/s10311-019-00959-wRammohan A., Reddy J. S., Sravya G., Rao C. N., Zyryanov G. V. Chalcone synthesis, properties and medicinal applications: a review. Environmental Chemistry Letters, 2020, vol. 18, no. 2, pp. 433–458. https://doi.org/10.1007/s10311-019-00959-wSynthesis and antibacterial evaluation of novel cationic chalcone derivatives possessing broad spectrum antibacterial activity / W.-C. Chu [et al.] // European Journal of Medicinal Chemistry. – 2018. – Vol. 143 – P. 905–921. https://doi.org/10.1016/j.ejmech.2017.12.009Chu W.-C., Bai P.-Y., Yang J.-Q., Cui D.-Y., Hua Y.-G., Yang Y., Yang Q.-Q., Zhang E. Qin S. Synthesis and antibacterial evaluation of novel cationic chalcone derivatives possessing broad spectrum antibacterial activity. European Journal of Medicinal Chemistry,2018, vol. 143, pp. 905–921. https://doi.org/10.1016/j.ejmech.2017.12.009Synthesis, crystal structure and antimicrobial potential of some fluorinated chalcone-1,2,3-triazole conjugates / P. Yadav [et al.] // European Journal of Medicinal Chemistry. – 2018. – Vol. 155. – P. 263–274. https://doi.org/10.1016/j.ejmech.2018.05.055Yadav P., Lal K., Kumar L., Kumar A., Kumar A., Paul A. K., Kumar R. Synthesis, crystal structure and antimicrobial potential of some fluorinated chalcone-1,2,3-triazole conjugates. European Journal of Medicinal Chemistry, 2018. vol. 155, pp. 263–274. https://doi.org/10.1016/j.ejmech.2018.05.055Microwave assisted synthesis of chalcone and its polycyclic heterocyclic analogues as promising antibacterial agents: In vitro, in silico and DFT studies / S. A. Khan [et al.] // Journal of Molecular Structure. – 2019. – Vol. 1190 – P. 77–85. https://doi.org/10.1016/j.molstruc.2019.04.046Khan S. A., Asiri A.M., Al-Ghamdi N. S. M., Asad M., Zayed M. E. M., Elroby S. A. K., Aqlan F. M., Wani M. Y., Sharma K. Microwave assisted synthesis of chalcone and its polycyclic heterocyclic analogues as promising antibacterial agents: In vitro, in silico and DFT studies. Journal of Molecular Structure, 2019, vol. 1190, pp. 77–85. https://doi.org/10.1016/j.molstruc.2019.04.046Synthesis and Utility of α,β-Unsaturated Ketone Bearing Naphthalene and Benzofuran Rings in the Synthesis of Some N -heterocycles with Their Antiviral and Antitumor Activity Evaluation: Synthesis and Utility of Naphthalene-Benzofuran Chalcone in the Synthesis of New Heterocycles / R. S. Gouhar [et al.] // J. Heterocyclic Chem. – 2018. – Vol. 55, N 10. – P. 2368–2380. https://doi.org/10.1002/jhet.3301Gouhar R. S., Ewies E. F., El-Shehry M. F., Shaheen M. N. F., Ibrahim E.-M. M. E. Synthesis and Utility of α,β-Unsaturated Ketone Bearing Naphthalene and Benzofuran Rings in the Synthesis of Some N -heterocycles with Their Antiviral and Antitumor Activity Evaluation: Synthesis and Utility of Naphthalene-Benzofuran Chalcone in the Synthesis of New Heterocycles. Journal of Heterocyclic Chemistry, 2018, vol. 55, pp. 2368–2380. https://doi.org/10.1002/jhet.3301Design, Synthesis, and Biological Evaluation of Novel Pyrazole, Oxazole, and Pyridine Derivatives as Potential Anticancer Agents Using Mixed Chalcone / M. H. Ahmed [et al.] // J. Heterocyclic Chem. – 2019. – Vol. 56, N 1. – P. 114–123. https://doi.org/10.1002/jhet.3380Ahmed M. H., El‐Hashash M. A., Marzouk M. I., El‐Naggar A. M. Design, Synthesis, and Biological Evaluation of Novel Pyrazole, Oxazole, and Pyridine Derivatives as Potential Anticancer Agents Using Mixed Chalcone. Journal of Heterocyclic Chemistry, 2019, vol. 56, pp. 114–123. https://doi.org/10.1002/jhet.3380Pyrimidine candidate as promising scaffold and their biological evaluation / J. Alam [et al.] // Int. J. Pharmacol. Pharm. Sci. – 2015. – Vol. 2, N 4. – P. 55–69.Alam J., Alam O., Shrivastava N., Naim M., Alam P. Pyrimidine candidate as promising scaffold and their biological evaluation. International Journal of Pharmacology and Pharmaceutical Sciences, 2015, vol. 2, no. 4, pp. 55–69.Синтез и противомикробная активность халконов с бензотриазолилметильными и имидазолилметильными заместителями / Л. В. Тинь [и др.] // ЖОрХ. – 2014. – Т. 50, № 12. – С. 1786–1793.Chinh L V., Hung T. N., Nga N. T., Hang T. T. N., Mai T. T. N. Tarasevich V. A. Synthesis and antimicrobial activity of chalcones containing benzotriazolylmethyl and imidazolylmethyl substituents. Russian Journal of Organic Chemistry, 2014, vol. 50, no. 12, pp. 1767–1774. https://doi.org/ 10.1134/S1070428014120094Synthesis, antiviral, antituberculostic, and antibacterial activities of some novel, 4-(4-substituted phenyl)-6-(4-nitrophenyl)-2-(substituted imino)pyrimidines / A. A. Siddiqui [et al.] // Arch. Pharm. Chem. – 2007. – Vol. 340, N 2. – P. 95–102. https://doi.org/10.1002/ardp.200600121Siddiqui A. A., Rajesh R., Mojahid-Ul-Islam, Alagarsamy V., De Clercq E. Synthesis, Antiviral, Antituberculostic, and Antibacterial Activities of Some Novel, 4-(4-substituted phenyl)-6-(4-nitrophenyl)-2-(substituted imino)pyrimidines. Archiv der Pharmazie – Chemistry in Life Sciences, 2007, vol. 340, no. 2, pp. 95–102. https://doi.org/10.1002/ardp.200600121

The authors declare that there are no conflicts of interest present.