Schiff Bases of Isatin and Adamantane-1-Carbohydrazide: Synthesis, Characterization and Anticonvulsant Activity
Epilepsy is the most common neurological condition and cause of substantial morbidity and mortality. In the present study, the molecular hybridization tool was adopted to obtain six Schiff bases of isatin and adamantane-1-carbohydrazide (18–23). Then, their anticonvulsant activity was evaluated usin...
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| Format: | Article |
| Language: | English |
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Wiley
2021-01-01
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| Series: | Journal of Chemistry |
| Online Access: | http://dx.doi.org/10.1155/2021/6659156 |
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| author | Hind M. Osman Tilal Elsaman Bashir A. Yousef Esraa Elhadi Aimun A. E. Ahmed Eyman Mohamed Eltayib Malik Suliman Mohamed Magdi Awadalla Mohamed |
| author_facet | Hind M. Osman Tilal Elsaman Bashir A. Yousef Esraa Elhadi Aimun A. E. Ahmed Eyman Mohamed Eltayib Malik Suliman Mohamed Magdi Awadalla Mohamed |
| author_sort | Hind M. Osman |
| collection | DOAJ |
| description | Epilepsy is the most common neurological condition and cause of substantial morbidity and mortality. In the present study, the molecular hybridization tool was adopted to obtain six Schiff bases of isatin and adamantane-1-carbohydrazide (18–23). Then, their anticonvulsant activity was evaluated using pentylenetetrazole- (PTZ-) induced seizure model using phenobarbitone as a positive control. Our findings showed that compounds 18–23 provided significant protection against PTZ-induced seizure, and maximum activities were associated with compound 23. Moreover, all investigated compounds increased the latency of induced convulsion and reduced the duration of epilepsy with compound 23 being the best. Interestingly, most of the synthesized molecules showed reduction in neurological symptoms and severity of the seizure. Molecular docking studies suggest GABA-A receptor as a potential target, and in silico ADME screening revealed that the pharmaceutical properties of compound 23 are within the specified limit. Thus, compound 23 was identified as a promising candidate that warrants further drug discovery processes. |
| format | Article |
| id | doaj-art-8d4216d88e854d8a992717af64e2d67c |
| institution | Kabale University |
| issn | 2090-9063 2090-9071 |
| language | English |
| publishDate | 2021-01-01 |
| publisher | Wiley |
| record_format | Article |
| series | Journal of Chemistry |
| spelling | doaj-art-8d4216d88e854d8a992717af64e2d67c2025-08-20T03:37:54ZengWileyJournal of Chemistry2090-90632090-90712021-01-01202110.1155/2021/66591566659156Schiff Bases of Isatin and Adamantane-1-Carbohydrazide: Synthesis, Characterization and Anticonvulsant ActivityHind M. Osman0Tilal Elsaman1Bashir A. Yousef2Esraa Elhadi3Aimun A. E. Ahmed4Eyman Mohamed Eltayib5Malik Suliman Mohamed6Magdi Awadalla Mohamed7Department of Pharmaceutical Chemistry, College of Pharmacy, Omdurman Islamic University, Omdurman, SudanDepartment of Pharmaceutical Chemistry, College of Pharmacy, Omdurman Islamic University, Omdurman, SudanDepartment of Pharmacology, Faculty of Pharmacy, University of Khartoum, Khartoum, SudanDepartment of Pharmacology, School of Pharmaceutical Sciences, China Pharmaceutical University, Nanjing, ChinaDepartment of Pharmacology, College of Pharmacy, Omdurman Islamic University, Omdurman, SudanDepartment of Pharmaceutics, College of Pharmacy, Jouf University, Sakaka, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, Jouf University, Sakaka, Saudi ArabiaDepartment of Pharmaceutical Chemistry, College of Pharmacy, Jouf University, Sakaka, Saudi ArabiaEpilepsy is the most common neurological condition and cause of substantial morbidity and mortality. In the present study, the molecular hybridization tool was adopted to obtain six Schiff bases of isatin and adamantane-1-carbohydrazide (18–23). Then, their anticonvulsant activity was evaluated using pentylenetetrazole- (PTZ-) induced seizure model using phenobarbitone as a positive control. Our findings showed that compounds 18–23 provided significant protection against PTZ-induced seizure, and maximum activities were associated with compound 23. Moreover, all investigated compounds increased the latency of induced convulsion and reduced the duration of epilepsy with compound 23 being the best. Interestingly, most of the synthesized molecules showed reduction in neurological symptoms and severity of the seizure. Molecular docking studies suggest GABA-A receptor as a potential target, and in silico ADME screening revealed that the pharmaceutical properties of compound 23 are within the specified limit. Thus, compound 23 was identified as a promising candidate that warrants further drug discovery processes.http://dx.doi.org/10.1155/2021/6659156 |
| spellingShingle | Hind M. Osman Tilal Elsaman Bashir A. Yousef Esraa Elhadi Aimun A. E. Ahmed Eyman Mohamed Eltayib Malik Suliman Mohamed Magdi Awadalla Mohamed Schiff Bases of Isatin and Adamantane-1-Carbohydrazide: Synthesis, Characterization and Anticonvulsant Activity Journal of Chemistry |
| title | Schiff Bases of Isatin and Adamantane-1-Carbohydrazide: Synthesis, Characterization and Anticonvulsant Activity |
| title_full | Schiff Bases of Isatin and Adamantane-1-Carbohydrazide: Synthesis, Characterization and Anticonvulsant Activity |
| title_fullStr | Schiff Bases of Isatin and Adamantane-1-Carbohydrazide: Synthesis, Characterization and Anticonvulsant Activity |
| title_full_unstemmed | Schiff Bases of Isatin and Adamantane-1-Carbohydrazide: Synthesis, Characterization and Anticonvulsant Activity |
| title_short | Schiff Bases of Isatin and Adamantane-1-Carbohydrazide: Synthesis, Characterization and Anticonvulsant Activity |
| title_sort | schiff bases of isatin and adamantane 1 carbohydrazide synthesis characterization and anticonvulsant activity |
| url | http://dx.doi.org/10.1155/2021/6659156 |
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