Design and Synthesis of Sustain-Acting Melatonin Prodrugs
Twelve melatonin amide prodrugs aiming at prolonging the action of melatonin in vivo by improving its half-life were designed and synthesized. Using an 80% human plasma model, it was found that the aliphatic amide derivatives were relatively stable and melatonin release from these compounds was not...
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| Format: | Article |
| Language: | English |
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Wiley
2013-01-01
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| Series: | Journal of Chemistry |
| Online Access: | http://dx.doi.org/10.1155/2013/684760 |
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| author | Phạm Văn Thoại Nguyen Hai Nam |
| author_facet | Phạm Văn Thoại Nguyen Hai Nam |
| author_sort | Phạm Văn Thoại |
| collection | DOAJ |
| description | Twelve melatonin amide prodrugs aiming at prolonging the action of melatonin in vivo by improving its half-life were designed and synthesized. Using an 80% human plasma model, it was found that the aliphatic amide derivatives were relatively stable and melatonin release from these compounds was not sufficient with melatonin release percentage. After 4-hour incubation with 80% human plasma, the melatonin release percentage achieved only approximately less than 20%. In contrast, the -succinyl and -glutaroylmelatonin derivatives (compounds 11 and 12, resp.) were found to release melatonin in much higher rates. After 3-hour incubation in 80% human plasma, the melatonin release rates from 11 and 12 were found to be 67.3 and 75.6%, respectively. From these results, the -succinyl and -glutaroylmelatonin derivatives (compounds 11 and 12) could be promising as sustained release prodrugs of melatonin. |
| format | Article |
| id | doaj-art-9b5668250053495b84117e7ff0ee2c4a |
| institution | Kabale University |
| issn | 2090-9063 2090-9071 |
| language | English |
| publishDate | 2013-01-01 |
| publisher | Wiley |
| record_format | Article |
| series | Journal of Chemistry |
| spelling | doaj-art-9b5668250053495b84117e7ff0ee2c4a2025-08-20T03:36:58ZengWileyJournal of Chemistry2090-90632090-90712013-01-01201310.1155/2013/684760684760Design and Synthesis of Sustain-Acting Melatonin ProdrugsPhạm Văn Thoại0Nguyen Hai Nam1Department of Pharmaceutical Chemistry, Hanoi University of Pharmacy, 13-15 Le Thanh Tong, Hanoi, VietnamDepartment of Pharmaceutical Chemistry, Hanoi University of Pharmacy, 13-15 Le Thanh Tong, Hanoi, VietnamTwelve melatonin amide prodrugs aiming at prolonging the action of melatonin in vivo by improving its half-life were designed and synthesized. Using an 80% human plasma model, it was found that the aliphatic amide derivatives were relatively stable and melatonin release from these compounds was not sufficient with melatonin release percentage. After 4-hour incubation with 80% human plasma, the melatonin release percentage achieved only approximately less than 20%. In contrast, the -succinyl and -glutaroylmelatonin derivatives (compounds 11 and 12, resp.) were found to release melatonin in much higher rates. After 3-hour incubation in 80% human plasma, the melatonin release rates from 11 and 12 were found to be 67.3 and 75.6%, respectively. From these results, the -succinyl and -glutaroylmelatonin derivatives (compounds 11 and 12) could be promising as sustained release prodrugs of melatonin.http://dx.doi.org/10.1155/2013/684760 |
| spellingShingle | Phạm Văn Thoại Nguyen Hai Nam Design and Synthesis of Sustain-Acting Melatonin Prodrugs Journal of Chemistry |
| title | Design and Synthesis of Sustain-Acting Melatonin Prodrugs |
| title_full | Design and Synthesis of Sustain-Acting Melatonin Prodrugs |
| title_fullStr | Design and Synthesis of Sustain-Acting Melatonin Prodrugs |
| title_full_unstemmed | Design and Synthesis of Sustain-Acting Melatonin Prodrugs |
| title_short | Design and Synthesis of Sustain-Acting Melatonin Prodrugs |
| title_sort | design and synthesis of sustain acting melatonin prodrugs |
| url | http://dx.doi.org/10.1155/2013/684760 |
| work_keys_str_mv | AT phamvanthoai designandsynthesisofsustainactingmelatoninprodrugs AT nguyenhainam designandsynthesisofsustainactingmelatoninprodrugs |