Pharmacological Properties of Sulfonamide Derivatives, New Inhibitors of Carbonic Anhydrase

Selective blocking of individual isoforms of carbonic anhydrase (CA) is now one of the main directions in the development of its inhibitors. The new 1,2,4-oxadiazole-containing sulfonamides B12 and B13 predominantly block CA II and CA IX. The study of acute toxicity of B12 and B13 showed their safet...

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Published in:Bulletin of experimental biology and medicine Vol. 175; no. 2; pp. 205 - 209
Main Authors: Khokhlov, A. L., Shetnev, A. A., Korsakov, M. K., Fedorov, V. N., Tyushina, A. N., Volkhin, N. N., Vdovichenko, V. P.
Format: Journal Article
Language:English
Published: New York Springer US 01.06.2023
Springer
Springer Nature B.V
Subjects:
Acute toxicity
Analysis
Animals
Antibiotics
Antidepressants
Antigens, Neoplasm
Biomedical and Life Sciences
Biomedicine
Brinzolamide
Carbon dioxide
Carbonic Anhydrase Inhibitors - pharmacology
Carbonic anhydrases
Carbonic Anhydrases - metabolism
Cell Biology
Drugs
Enzymes
Glaucoma
Internal Medicine
Isoforms
Laboratory animals
Laboratory Medicine
Medical practices
Pathology
Pedagogy
Pharmaceuticals
Physiology
Protein Isoforms
Rabbits
Respiration
Structure-Activity Relationship
Sulfonamides
Sulfonamides - pharmacology
Toxicology
carbonic anhydrases
sulfonamides
carbonic anhydrase inhibitors
intraocular pressure
ISSN:0007-4888, 1573-8221, 1573-8221
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Abstract Selective blocking of individual isoforms of carbonic anhydrase (CA) is now one of the main directions in the development of its inhibitors. The new 1,2,4-oxadiazole-containing sulfonamides B12 and B13 predominantly block CA II and CA IX. The study of acute toxicity of B12 and B13 showed their safety. Substance B13 caused a relatively short-term, but rapid (within 30 min) decrease in the intraocular pressure in rabbits, which indicates the promise of its use for the emergency decrease in the intraocular pressure in medical practice. Analysis of the effects of sulfonamides on the functions of CNS showed that compound B12 probably exhibit tranquilizing activity; B13 is promising for the creation of drugs that have an antidepressant effect and at the same time increase the mental and physical performance.
AbstractList Selective blocking of individual isoforms of carbonic anhydrase (CA) is now one of the main directions in the development of its inhibitors. The new 1,2,4-oxadiazole-containing sulfonamides B12 and B13 predominantly block CA II and CA IX. The study of acute toxicity of B12 and B13 showed their safety. Substance B13 caused a relatively short-term, but rapid (within 30 min) decrease in the intraocular pressure in rabbits, which indicates the promise of its use for the emergency decrease in the intraocular pressure in medical practice. Analysis of the effects of sulfonamides on the functions of CNS showed that compound B12 probably exhibit tranquilizing activity; B13 is promising for the creation of drugs that have an antidepressant effect and at the same time increase the mental and physical performance.Selective blocking of individual isoforms of carbonic anhydrase (CA) is now one of the main directions in the development of its inhibitors. The new 1,2,4-oxadiazole-containing sulfonamides B12 and B13 predominantly block CA II and CA IX. The study of acute toxicity of B12 and B13 showed their safety. Substance B13 caused a relatively short-term, but rapid (within 30 min) decrease in the intraocular pressure in rabbits, which indicates the promise of its use for the emergency decrease in the intraocular pressure in medical practice. Analysis of the effects of sulfonamides on the functions of CNS showed that compound B12 probably exhibit tranquilizing activity; B13 is promising for the creation of drugs that have an antidepressant effect and at the same time increase the mental and physical performance.
Selective blocking of individual isoforms of carbonic anhydrase (CA) is now one of the main directions in the development of its inhibitors. The new 1,2,4-oxadiazole-containing sulfonamides B12 and B13 predominantly block CA II and CA IX. The study of acute toxicity of B12 and B13 showed their safety. Substance B13 caused a relatively short-term, but rapid (within 30 min) decrease in the intraocular pressure in rabbits, which indicates the promise of its use for the emergency decrease in the intraocular pressure in medical practice. Analysis of the effects of sulfonamides on the functions of CNS showed that compound B12 probably exhibit tranquilizing activity; B13 is promising for the creation of drugs that have an antidepressant effect and at the same time increase the mental and physical performance.
Selective blocking of individual isoforms of carbonic anhydrase (CA) is now one of the main directions in the development of its inhibitors. The new 1,2,4-oxadiazole-containing sulfonamides B12 and B13 predominantly block CA II and CA IX. The study of acute toxicity of B12 and B13 showed their safety. Substance B13 caused a relatively short-term, but rapid (within 30 min) decrease in the intraocular pressure in rabbits, which indicates the promise of its use for the emergency decrease in the intraocular pressure in medical practice. Analysis of the effects of sulfonamides on the functions of CNS showed that compound B12 probably exhibit tranquilizing activity; B13 is promising for the creation of drugs that have an antidepressant effect and at the same time increase the mental and physical performance. Key Words: carbonic anhydrases; carbonic anhydrase inhibitors; sulfonamides; intraocular pressure
Audience Academic
Author Korsakov, M. K.
Tyushina, A. N.
Volkhin, N. N.
Shetnev, A. A.
Fedorov, V. N.
Vdovichenko, V. P.
Khokhlov, A. L.
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Cites_doi 10.3109/14756366.2015.1122001
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10.1080/13543776.2018.1519023
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10.1016/j.bioorg.2019.103557
10.1017/CBO9781139344319
10.1016/j.ejmech.2019.02.044
10.1124/jpet.110.167270
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Keywords carbonic anhydrases
sulfonamides
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intraocular pressure
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References_xml – reference: Ghorai S, Pulya S, Ghosh K, Panda P, Ghosh B, Gayen S. Structure-activity relationship of human carbonic anhydrase-II inhibitors: Detailed insight for future development as anti-glaucoma agents. Bioorg. Chem. 2020;95:103557. doi: https://doi.org/10.1016/j.bioorg.2019.103557
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SubjectTerms Acute toxicity
Analysis
Animals
Antibiotics
Antidepressants
Antigens, Neoplasm
Biomedical and Life Sciences
Biomedicine
Brinzolamide
Carbon dioxide
Carbonic Anhydrase Inhibitors - pharmacology
Carbonic anhydrases
Carbonic Anhydrases - metabolism
Cell Biology
Drugs
Enzymes
Glaucoma
Internal Medicine
Isoforms
Laboratory animals
Laboratory Medicine
Medical practices
Pathology
Pedagogy
Pharmaceuticals
Physiology
Protein Isoforms
Rabbits
Respiration
Structure-Activity Relationship
Sulfonamides
Sulfonamides - pharmacology
Toxicology
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