Structure-based design, synthesis, and anticonvulsant activity of isatin-1-N-phenylacetamide derivatives
| Autor: | Li-Ping Guan, Chao Xie, Li-Ming Tang, Cheng-Yan Pan, Si-Hong Wang, Fu-Nan Li |
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| Rok vydání: | 2013 |
| Předmět: |
Stereochemistry
Chemistry medicine.medical_treatment Isatin Organic Chemistry Neurotoxicity Carbamazepine Pharmacology medicine.disease Anticonvulsant Agent chemistry.chemical_compound Anticonvulsant In vivo medicine Phenobarbital General Pharmacology Toxicology and Pharmaceutics Pharmacophore medicine.drug |
| Zdroj: | Medicinal Chemistry Research. 23:2161-2168 |
| ISSN: | 1554-8120 1054-2523 |
| DOI: | 10.1007/s00044-013-0811-1 |
| Popis: | In an effort to develop the potent anticonvulsant agents, a series of novel isatin-1-N-phenylacetamide derivatives was synthesized and screened for their in vivo anticonvulsant activity against maximal electroshock test and evaluated for their neurotoxicity by the rotarod test at the same dose levels. Ten compounds exhibited the anticonvulsant activity. 2-(5-Methyl-2,3-dioxoindolin-1-yl)-N-phenylacetamide (4b) was found to be the most potent compound of the series with an ED50 of 91.3 mg/kg, TD50 of >1,000 mg/kg, a higher protective index (PI = TD50/ED50, >11) was gained than the reference drug phenobarbital and carbamazepine. The essential structural features responsible for interaction with receptor site are established within a suggested pharmacophore. |
| Databáze: | OpenAIRE |
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