Antihypoxic Activity of 2,5-diaryl-8,8-dimethyl-3,6,7,8-tetrahydro-2<i>H</i>-pyrido[4,3,2-<i>de</i>]quinnolin-3-ones
Introduction. The state of hypoxia, causing damage and cell death, underlies many pathological processes. In addition, hypoxia induces a state of free radical oxidation, which enhances the damaging effect of hypoxic damage. This necessitates the synthesis of new compounds and the creation on their b...
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| Format: | Article |
| Language: | Russian |
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LLC Center of Pharmaceutical Analytics (LLC «CPHA»)
2022-12-01
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| Series: | Разработка и регистрация лекарственных средств |
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| Online Access: | https://www.pharmjournal.ru/jour/article/view/1389 |
| _version_ | 1797874898515787776 |
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| author | S. S. Zykova K. V. Namyatova K. L. Gankova E. A. Lystsova T. V. Shavrina S. N. Shurov |
| author_facet | S. S. Zykova K. V. Namyatova K. L. Gankova E. A. Lystsova T. V. Shavrina S. N. Shurov |
| author_sort | S. S. Zykova |
| collection | DOAJ |
| description | Introduction. The state of hypoxia, causing damage and cell death, underlies many pathological processes. In addition, hypoxia induces a state of free radical oxidation, which enhances the damaging effect of hypoxic damage. This necessitates the synthesis of new compounds and the creation on their basis of drugs with antihypoxic activity.Aim. The aim of this study is the synthesis and study of the antihypoxic activity of 2,5-diaryl-8,8-dimethyl-3,6,7,8-tetrahydro-2Н-pyrido[4,3,2-de] quinnolin-3-ones.Materials and methods. Compounds of the 2,5-diaryl-8,8-dimethyl-3,6,7,8-tetrahydro-2H-pyrido[4,3,2-de]quinnolin-3-ones series were obtained as a result of the interaction of 2-aryl-7,7-dimethyl-5-oxo-5,6,7,8-tetrahydroquinoline-4-carboxylic acids c o-tolyl-, p-tolyl-, p-fluoro-, p-nitro-, 2,4,6-trichlorophenylhydrazines. As a result, 10 substances were synthesized, the structure of which was confirmed by IR and 1H NMR spectroscopy. The study of the antihypoxic activity of the obtained compounds was carried out using the method of normobaric hypoxia with hypercapnia («hypoxia in a jar»).Results and discussion. The studied compounds have different effects on the lifespan of mice under conditions of acute normobaric hypoxia with hypercapnia. Compounds IIIi and IIId, respectively, increased the lifespan of mice most significantly by 26.36 % and 25.64 %, respectively, compounds IIIa, IIIb, IIIg were less significant, compounds IIIc and IIIf had no effect, and compound IIIj had a prohypoxic effect.Conclusion. Compounds with the most pronounced antihypoxic and antioxidant properties have been identified. Thus, further synthesis and study of 2,5-diaryl-8,8-dimethyl-3,6,7,8-tetrahydro-2H-pyrido[4,3,2-de]cinnolin-3-ones is reasonable. |
| first_indexed | 2024-04-10T01:39:22Z |
| format | Article |
| id | doaj.art-95b32629369a4e4a8ab1fba4edd5d86f |
| institution | Directory Open Access Journal |
| issn | 2305-2066 2658-5049 |
| language | Russian |
| last_indexed | 2024-04-10T01:39:22Z |
| publishDate | 2022-12-01 |
| publisher | LLC Center of Pharmaceutical Analytics (LLC «CPHA») |
| record_format | Article |
| series | Разработка и регистрация лекарственных средств |
| spelling | doaj.art-95b32629369a4e4a8ab1fba4edd5d86f2023-03-13T09:14:04ZrusLLC Center of Pharmaceutical Analytics (LLC «CPHA»)Разработка и регистрация лекарственных средств2305-20662658-50492022-12-01114222610.33380/2305-2066-2022-11-4(1)-22-261045Antihypoxic Activity of 2,5-diaryl-8,8-dimethyl-3,6,7,8-tetrahydro-2<i>H</i>-pyrido[4,3,2-<i>de</i>]quinnolin-3-onesS. S. Zykova0K. V. Namyatova1K. L. Gankova2E. A. Lystsova3T. V. Shavrina4S. N. Shurov5ФГБОУ ВО «Пермская государственная фармацевтическая академия» Министерства здравоохранения Российской Федерации (ФГБОУ ВО ПГФА Минздрава России)ФГБОУ ВО «Пермская государственная фармацевтическая академия» Министерства здравоохранения Российской Федерации (ФГБОУ ВО ПГФА Минздрава России)ФГБОУ ВО «Пермская государственная фармацевтическая академия» Министерства здравоохранения Российской Федерации (ФГБОУ ВО ПГФА Минздрава России)ФГАОУ ВО «Пермский государственный национальный исследовательский университет» (ПГНИУ)ФГАОУ ВО «Пермский государственный национальный исследовательский университет» (ПГНИУ)ФГАОУ ВО «Пермский государственный национальный исследовательский университет» (ПГНИУ)Introduction. The state of hypoxia, causing damage and cell death, underlies many pathological processes. In addition, hypoxia induces a state of free radical oxidation, which enhances the damaging effect of hypoxic damage. This necessitates the synthesis of new compounds and the creation on their basis of drugs with antihypoxic activity.Aim. The aim of this study is the synthesis and study of the antihypoxic activity of 2,5-diaryl-8,8-dimethyl-3,6,7,8-tetrahydro-2Н-pyrido[4,3,2-de] quinnolin-3-ones.Materials and methods. Compounds of the 2,5-diaryl-8,8-dimethyl-3,6,7,8-tetrahydro-2H-pyrido[4,3,2-de]quinnolin-3-ones series were obtained as a result of the interaction of 2-aryl-7,7-dimethyl-5-oxo-5,6,7,8-tetrahydroquinoline-4-carboxylic acids c o-tolyl-, p-tolyl-, p-fluoro-, p-nitro-, 2,4,6-trichlorophenylhydrazines. As a result, 10 substances were synthesized, the structure of which was confirmed by IR and 1H NMR spectroscopy. The study of the antihypoxic activity of the obtained compounds was carried out using the method of normobaric hypoxia with hypercapnia («hypoxia in a jar»).Results and discussion. The studied compounds have different effects on the lifespan of mice under conditions of acute normobaric hypoxia with hypercapnia. Compounds IIIi and IIId, respectively, increased the lifespan of mice most significantly by 26.36 % and 25.64 %, respectively, compounds IIIa, IIIb, IIIg were less significant, compounds IIIc and IIIf had no effect, and compound IIIj had a prohypoxic effect.Conclusion. Compounds with the most pronounced antihypoxic and antioxidant properties have been identified. Thus, further synthesis and study of 2,5-diaryl-8,8-dimethyl-3,6,7,8-tetrahydro-2H-pyrido[4,3,2-de]cinnolin-3-ones is reasonable.https://www.pharmjournal.ru/jour/article/view/13892,5-диарил-8,8-диметил-3,6,7,8-тетрагидро-2<i>н</i>-пиридо[4,3,2-<i>de</i>]хиннолин-3-оныантигипоксическая активностьтрициклические гетероциклынормобарическая гипоксиягиперкапния |
| spellingShingle | S. S. Zykova K. V. Namyatova K. L. Gankova E. A. Lystsova T. V. Shavrina S. N. Shurov Antihypoxic Activity of 2,5-diaryl-8,8-dimethyl-3,6,7,8-tetrahydro-2<i>H</i>-pyrido[4,3,2-<i>de</i>]quinnolin-3-ones Разработка и регистрация лекарственных средств 2,5-диарил-8,8-диметил-3,6,7,8-тетрагидро-2<i>н</i>-пиридо[4,3,2-<i>de</i>]хиннолин-3-оны антигипоксическая активность трициклические гетероциклы нормобарическая гипоксия гиперкапния |
| title | Antihypoxic Activity of 2,5-diaryl-8,8-dimethyl-3,6,7,8-tetrahydro-2<i>H</i>-pyrido[4,3,2-<i>de</i>]quinnolin-3-ones |
| title_full | Antihypoxic Activity of 2,5-diaryl-8,8-dimethyl-3,6,7,8-tetrahydro-2<i>H</i>-pyrido[4,3,2-<i>de</i>]quinnolin-3-ones |
| title_fullStr | Antihypoxic Activity of 2,5-diaryl-8,8-dimethyl-3,6,7,8-tetrahydro-2<i>H</i>-pyrido[4,3,2-<i>de</i>]quinnolin-3-ones |
| title_full_unstemmed | Antihypoxic Activity of 2,5-diaryl-8,8-dimethyl-3,6,7,8-tetrahydro-2<i>H</i>-pyrido[4,3,2-<i>de</i>]quinnolin-3-ones |
| title_short | Antihypoxic Activity of 2,5-diaryl-8,8-dimethyl-3,6,7,8-tetrahydro-2<i>H</i>-pyrido[4,3,2-<i>de</i>]quinnolin-3-ones |
| title_sort | antihypoxic activity of 2 5 diaryl 8 8 dimethyl 3 6 7 8 tetrahydro 2 i h i pyrido 4 3 2 i de i quinnolin 3 ones |
| topic | 2,5-диарил-8,8-диметил-3,6,7,8-тетрагидро-2<i>н</i>-пиридо[4,3,2-<i>de</i>]хиннолин-3-оны антигипоксическая активность трициклические гетероциклы нормобарическая гипоксия гиперкапния |
| url | https://www.pharmjournal.ru/jour/article/view/1389 |
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