Yaroslavl, Yaroslavl, Russian Federation
Yaroslavl, Yaroslavl, Russian Federation
Moscow Institute of Physics and Technology (State University)
from 01.01.2024 until now
Yaroslavl, Yaroslavl, Russian Federation
Yaroslavl, Yaroslavl, Russian Federation
Glaucoma is the leading cause of irreversible blindness. Early diagnosis and effective treatment can reduce the progression of the disease and prevent irreversible decay of visual functions. Indeed, human carboanhydrase isoform II is a classical target for glaucoma treatment. We proposed a compound molecule 5 (5 trifluoromethyl-isoxazol-3-yl)furan-2-sulfonamide under the project name B016, which showed high activity as a human carboanhydrase II inhibitor by in vitro tests. Our team is currently conducting development and preclinical studies of a medicinal product in the eye drops form based on this compound. One of the stages of pharmaceutical research is the development of quality control methods for both the pharmaceutical substance and the finished dosage form. We have developed a chromatographic separation procedure, which can be used for quality control of active pharmaceutical substance by quantification indicators. We also determined the impurity profile, i.e. the structure of the impurities found in the reaction product of compound B016.
carboanhydrase, glaucoma, quality control, impurity profile, high-performance liquid chromatography
1. Schellack, N., Schellack, G. & Bezuidenhout, S. (2015) Glaucoma: A brief review, SA Pharmaceutical Journal, (82), pp. 18-22. DOI: 10520/EJC174862.
2. Kurysheva, N.I. (2020) Carboanhydrase inhibitors in glaucoma treatment. Review. Part 1, Oftal`mologiya, 17(3), pp. 542-549. DOI:https://doi.org/10.18008/1816-5095-2020-3S-542-549 (in Russian).
3. Kurysheva, N.I. (2020) Carboanhydrase inhibitors in glaucoma treatment. Review. Part 2, Oftal`mologiya, 17(4), pp. 676-682. DOI:https://doi.org/10.18008/1816-5095-2020-4-676-682 (in Russian).
4. Scozzafava, A. & Mastrolorenzo, C.T. (2006) Supuran. Carbonic anhydrase inhibitors and activators and their use in therapy, Expert Opin. Ther., (16), pp. 1627-1664. DOI:https://doi.org/10.1517/13543776.16.12.1627.
5. Krylov, E.N. & Virzum L.V. (2021) Quantum chemical analysis of the interaction of alkylarylsulfonamides with α-carboanhydrase HCA II, Butlerovskie soobshheniya, 66(5), pp. 11-23. DOI:https://doi.org/10.37952/ROI-jbc-01/21-66-5-11 (in Russian).
6. Komshina, L.A., Martazova, V.V., Proskurina, I.K., Korsakov, M.K. & Kotov, A.D. (2020) Synthesis of 3 arylisoxazoles and their sulfamide derivatives, Butlerovskie soobshheniya, 63(9), pp.10-18. DOI:https://doi.org/10.37952/ROI-jbc-01/20-63-9-10 (in Russian).
7. Komshina, L.A., Vasilieva, E.A., Proskurina, I.K., Kotov, A.D. & Korsakov, M.K. (2021) Regioselectivity of sulfonyl chlorination of 3-aryl-5-N-acylaminoisoxazoles, Butlerovskie soobshheniya, 67(8), pp. 123-128. DOI:https://doi.org/10.37952/ROI: jbc-01/21-67-8-123 (in Russian).
8. Komshina, L.A., Vasilieva, E.A., Proskurina, I.K., Blumina, M.V., Kotov, A.D. & Korsakov, M.K. 2022. Regioselectivity of 1-Aryl-6-pyrazol-1-yl-pyridazines sulfonyl chlorination, Butlerovskie soobshheniya, 69(2), pp. 15-21. DOI:https://doi.org/10.37952/ROI: jbc-01/22-69-2-15 (in Russian).
9. Krasavin, M., Korsakov, M., Dorogov, M., Tuccinardi, T., Dedeoglu, N. & Supuran, C.T. (2015) Probing the «bipolar» nature of the carbonic anhydrase active site: Aromatic sulfonamides containing 1,3-oxazol-5-yl moiety as picomolar inhibitors of cytosolic CA I and CA II isoforms, Eur. J. Med. Chem., (101), pp. 334-347. DOI:https://doi.org/10.1016/j.ejmech.2015.06.022.
10. Krasavin, M., Korsakov, M., Zvonaryova, Z., Semyonychev, E., Tuccinardi, T., Kalinin, S. & Supuran, C.T. (2017) Human carbonic anhydrase inhibitory profile of mono- and bis-sulfonamides synthesized via a direct sulfochlorination of 3- and 4-(hetero)arylisoxazol-5-amine scaffolds, Bioorg. Med. Chem., 25(6), pp. 1914-1925. DOI:https://doi.org/10.1016/j.bmc.2017.02.018.
11. Dorogov, M.V. & Krasavin, M.Y. (2017) Aromatic derivatives of sulfonamides inhibitors of carboanhydrase II (CA II), their preparation and application methods. 2607630 RU (in Russian).
