Synthesis and evaluation of cerebroprotective activity of novel 6,7-dimethoxyquinazolin-4(3H)-one derivatives containing residues of amino acids and dipeptides
Neurodegenerative processes of the central nervous system are an important socially significant problem of modern society. They cause many diseases, such as Alzheimer's disease and cerebral ischemia, which significantly reduce the quality of human life and can lead to disability or death. The a...
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| Format: | Article |
| Language: | English |
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Uralʹskij federalʹnyj universitet imeni pervogo Prezidenta Rossii B.N. Elʹcina
2022-06-01
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| Series: | Chimica Techno Acta |
| Subjects: | |
| Online Access: | https://journals.urfu.ru/index.php/chimtech/article/view/5924 |
| _version_ | 1818114876899328000 |
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| author | Alexey S. Chiriapkin Ivan P. Kodonidi Dmitry I. Pozdnyakov |
| author_facet | Alexey S. Chiriapkin Ivan P. Kodonidi Dmitry I. Pozdnyakov |
| author_sort | Alexey S. Chiriapkin |
| collection | DOAJ |
| description | Neurodegenerative processes of the central nervous system are an important socially significant problem of modern society. They cause many diseases, such as Alzheimer's disease and cerebral ischemia, which significantly reduce the quality of human life and can lead to disability or death. The aim of this study was to synthesize novel 6,7-dimethoxyquinazolin-4(3H)-one derivatives with the remains of neuroactive amino acids and dipeptides in order to investigate their cerebroprotective properties. As a result of the study, 13 novel 6,7-dimetho-xyquinazolin-4(3H)-one derivatives were synthesized. Cerebral ischemia in rats was reproduced by irreversible right-sided occlusion of the middle cerebral artery using the Tamura method, and the area of brain necrosis was evaluated. Cognitive functions were evaluated in the Y-maze test. Among the studied quinazolinone derivatives, compounds 3i, 3j and 3k have the most pronounced cerebrotropic activity, which is not inferior to ethylmethylhydroxypyridine succinate in terms of pharmacological activity, making them promising objects for further research. |
| first_indexed | 2024-12-11T03:57:42Z |
| format | Article |
| id | doaj.art-9ee3996eaf2c46e5888f1cac903ed32c |
| institution | Directory Open Access Journal |
| issn | 2411-1414 |
| language | English |
| last_indexed | 2024-12-11T03:57:42Z |
| publishDate | 2022-06-01 |
| publisher | Uralʹskij federalʹnyj universitet imeni pervogo Prezidenta Rossii B.N. Elʹcina |
| record_format | Article |
| series | Chimica Techno Acta |
| spelling | doaj.art-9ee3996eaf2c46e5888f1cac903ed32c2022-12-22T01:21:44ZengUralʹskij federalʹnyj universitet imeni pervogo Prezidenta Rossii B.N. ElʹcinaChimica Techno Acta2411-14142022-06-019210.15826/chimtech.2022.9.2.124452Synthesis and evaluation of cerebroprotective activity of novel 6,7-dimethoxyquinazolin-4(3H)-one derivatives containing residues of amino acids and dipeptidesAlexey S. Chiriapkin0Ivan P. Kodonidi1Dmitry I. Pozdnyakov2Pyatigorsk Medical and Pharmaceutical Institute, Branch of Volgograd State Medical UniversityPyatigorsk Medical and Pharmaceutical Institute, Branch of Volgograd State Medical UniversityPyatigorsk Medical and Pharmaceutical Institute, Branch of Volgograd State Medical UniversityNeurodegenerative processes of the central nervous system are an important socially significant problem of modern society. They cause many diseases, such as Alzheimer's disease and cerebral ischemia, which significantly reduce the quality of human life and can lead to disability or death. The aim of this study was to synthesize novel 6,7-dimethoxyquinazolin-4(3H)-one derivatives with the remains of neuroactive amino acids and dipeptides in order to investigate their cerebroprotective properties. As a result of the study, 13 novel 6,7-dimetho-xyquinazolin-4(3H)-one derivatives were synthesized. Cerebral ischemia in rats was reproduced by irreversible right-sided occlusion of the middle cerebral artery using the Tamura method, and the area of brain necrosis was evaluated. Cognitive functions were evaluated in the Y-maze test. Among the studied quinazolinone derivatives, compounds 3i, 3j and 3k have the most pronounced cerebrotropic activity, which is not inferior to ethylmethylhydroxypyridine succinate in terms of pharmacological activity, making them promising objects for further research.https://journals.urfu.ru/index.php/chimtech/article/view/5924quinazolinonessynthesismedicinal chemistrycerebroprotective activityischemiaamino acidsdipeptides |
| spellingShingle | Alexey S. Chiriapkin Ivan P. Kodonidi Dmitry I. Pozdnyakov Synthesis and evaluation of cerebroprotective activity of novel 6,7-dimethoxyquinazolin-4(3H)-one derivatives containing residues of amino acids and dipeptides Chimica Techno Acta quinazolinones synthesis medicinal chemistry cerebroprotective activity ischemia amino acids dipeptides |
| title | Synthesis and evaluation of cerebroprotective activity of novel 6,7-dimethoxyquinazolin-4(3H)-one derivatives containing residues of amino acids and dipeptides |
| title_full | Synthesis and evaluation of cerebroprotective activity of novel 6,7-dimethoxyquinazolin-4(3H)-one derivatives containing residues of amino acids and dipeptides |
| title_fullStr | Synthesis and evaluation of cerebroprotective activity of novel 6,7-dimethoxyquinazolin-4(3H)-one derivatives containing residues of amino acids and dipeptides |
| title_full_unstemmed | Synthesis and evaluation of cerebroprotective activity of novel 6,7-dimethoxyquinazolin-4(3H)-one derivatives containing residues of amino acids and dipeptides |
| title_short | Synthesis and evaluation of cerebroprotective activity of novel 6,7-dimethoxyquinazolin-4(3H)-one derivatives containing residues of amino acids and dipeptides |
| title_sort | synthesis and evaluation of cerebroprotective activity of novel 6 7 dimethoxyquinazolin 4 3h one derivatives containing residues of amino acids and dipeptides |
| topic | quinazolinones synthesis medicinal chemistry cerebroprotective activity ischemia amino acids dipeptides |
| url | https://journals.urfu.ru/index.php/chimtech/article/view/5924 |
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