Synthesis and pharmacological evaluation of newer substituted benzoxazepine derivatives as potent anticonvulsant agents.
A series of 2-substitutedphenyl-3-(substitutedphenylamino)methyl-2,3-dihydro-4-diphenylamino-1,5-benzoxazepines (4a-4p) and 2-substitutedphenyl-3-substitutedphenylazo-2,3-dihydro-4-diphenylamino-1,5-benzoxazepines (5a-5p) have been synthesized from 2-substitutedphenyl-2,3-dihydro-4-diphenylamino-1,5-benzoxazepines (3a-3d) by the Mannich reaction and diazotization reaction, respectively. All these compounds were screened, in vivo, for their anticonvulsant activity and acute toxicity studies. Compounds 4p and 5p were found to be most potent compounds of this series and were compared with the reference drug phenytion sodium, lamotrigine and sodium valproate. The structures of these compounds have been established by IR, (1)H NMR and mass spectroscopic data.
Bajaj
Kiran
K
Medicinal Chemistry Division, Department of Pharmacology, Lala Lajpat Rai Memorial Medical College, Meerut, UP 250004, India.
Archana
Kumar
Ashok
A
D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis / Q000627:therapeutic use; D001552:Benzazepines / Q000138:chemical synthesis / Q000627:therapeutic use; D004305:Dose-Response Relationship, Drug; D004597:Electroshock; D000077213:Lamotrigine; D009682:Magnetic Resonance Spectroscopy; D010672:Phenytoin / Q000494:pharmacology; D012640:Seizures / Q000188:drug therapy*; D013329:Structure-Activity Relationship; D014227:Triazines / Q000494:pharmacology
D000927:Anticonvulsants; D001552:Benzazepines; D014227:Triazines; D010672:Phenytoin; D000077213:Lamotrigine