Synthesis and Anticonvulsant Activity of SomeN-Phenyl-2-phtalimidoethanesulfonamide Derivatives
| Autor: | Ozlem Akgul, Fatma Sultan Kilic, Kevser Erol, Varol Pabuccuoglu |
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| Rok vydání: | 2007 |
| Předmět: |
Male
Electroshock Sulfonamides Magnetic Resonance Spectroscopy Stereochemistry Chemistry medicine.medical_treatment Pharmaceutical Science Phthalimides Dose level Ring (chemistry) Mice Structure-Activity Relationship Taltrimide Anticonvulsant Seizures Drug Discovery Nitro medicine Animals Pentylenetetrazole Moiety Molecule Anticonvulsants Pharmacophore |
| Zdroj: | Archiv der Pharmazie. 340:656-660 |
| ISSN: | 1521-4184 0365-6233 |
| DOI: | 10.1002/ardp.200700166 |
| Popis: | In this study, inspired by the structures of the taltrimide, 2-phthalimidoethanesulphonamide, and the anilide pharmacophore known to be synthetically produced anticonvulsant compounds, fifteen N-phenyl-2-phtalimidoethanesulfonamide derivatives bearing substituents with diverse electronic and hydrophobic features on N-phenyl ring were synthesized. The structural confirmation of the title compounds was achieved by interpretation of spectral and analytical data. The anticonvulsant activity of the title compounds was determined against maximal electroshock seizure in mice at a dose level of 100 mg/kg. The preliminary screening results indicated that the exchange of the N-isopropyl moiety for an N-phenyl ring in the taltrimide molecule abolished the anticonvulsant activity. However, introducing certain substituents, such as nitro, methyl, and chloro, into the N-phenyl ring lead to more active compounds in comparison to the unsubstituted derivatives. |
| Databáze: | OpenAIRE |
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