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Design, synthesis and anticonvulsant activities of novel 1-(substituted/unsubstituted benzylidene)-4-(4-(6,8-dibromo-2-(methyl/phenyl)-4-oxoquinazolin-3(4H)-yl)phenyl) semicarbazide derivatives
- Source :
- Bioorganic & Medicinal Chemistry Letters. 22:3072-3078
- Publication Year :
- 2012
- Publisher :
- Elsevier BV, 2012.
-
Abstract
- Novel quinazolinone derivatives 5a-5n were designed, synthesized and screened for antiepileptic activity using MES and scPTZ seizures tests. Neurotoxicity study was performed by rotorod test. Compounds 5c, 5d, 5g, 5j and 5k were found active in the preliminary screening in MES model and/or scPTZ model. Further all these five compounds were administered to rats, 5c and 5d showed better activity than Phenytoin in oral route. Among all the title compounds tested, the most active one was 5c that revealed protection in MES at a dose of 30 mg/kg (ip) after 0.5 and 4h. This molecule also provided protection in the scPTZ at a dose of 100mg/kg (0.5h) and 300 mg/kg (4h).
- Subjects :
- Phenytoin
Stereochemistry
medicine.medical_treatment
Clinical Biochemistry
Pharmaceutical Science
Biochemistry
Structure-Activity Relationship
chemistry.chemical_compound
Seizures
Drug Discovery
medicine
Oral route
Animals
Structure–activity relationship
Molecular Biology
Quinazolinone
Quinazolinones
Semicarbazide
Schiff base
Dose-Response Relationship, Drug
Organic Chemistry
Rats
Semicarbazides
Anticonvulsant
chemistry
Design synthesis
Drug Design
Molecular Medicine
Anticonvulsants
Neurotoxicity Syndromes
medicine.drug
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 22
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....cbc990884aa277f21d454bee926e25e2
- Full Text :
- https://doi.org/10.1016/j.bmcl.2012.03.068