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Design and synthesis of anticonvulsants from a combined phthalimide–GABA–anilide and hydrazone pharmacophore
- Source :
- European Journal of Medicinal Chemistry. 42:146-151
- Publication Year :
- 2007
- Publisher :
- Elsevier BV, 2007.
-
Abstract
- Two series of pharmacophoric hybrids of phthalimide-GABA-anilides/hydrazones were designed and synthesized and evaluated for their anticonvulsant and neurotoxic properties. The structures of the synthesized compounds were confirmed by the use of their spectral data besides elemental analysis. Initial anticonvulsant screening was performed using intraperitoneal (i.p.) maximal electroshock-induced seizure (MES), subcutaneous pentylenetetrazole (scPTZ), subcutaneous strychnine (scSTY), and intraperitoneal picrotoxin (ipPIC)-induced seizure threshold tests. All of the compounds were ineffective in the MES test. Most of the compounds were found to be effective in the scSTY and ipPIC models and very few compounds showed protection in the scPTZ model.
- Subjects :
- Male
Stereochemistry
medicine.medical_treatment
Hydrazone
Phthalimides
Medicinal chemistry
Chemical synthesis
Phthalimide
Mice
Structure-Activity Relationship
chemistry.chemical_compound
Seizures
Drug Discovery
medicine
Animals
Anilides
gamma-Aminobutyric Acid
Pharmacology
chemistry.chemical_classification
Seizure threshold
Chemistry
Organic Chemistry
Hydrazones
Biological activity
General Medicine
Strychnine
Disease Models, Animal
Anticonvulsant
Rotarod Performance Test
Anticonvulsants
Pharmacophore
Subjects
Details
- ISSN :
- 02235234
- Volume :
- 42
- Database :
- OpenAIRE
- Journal :
- European Journal of Medicinal Chemistry
- Accession number :
- edsair.doi.dedup.....ddc76b3d131ae6383185f656b8efc643