Design & synthesis of 2-(substituted aryloxy)-5-(substituted benzylidene)-3-phenyl-2,5-dihydro-1H-[1,2,4] triazin-6-one as potential anticonvulsant agents.
A series of 2-(substituted aryloxy)-5-(substituted benzylidene)-3-phenyl-2,5-dihydro-1H-[1,2,4] triazin-6-one were designed & synthesized using appropriate synthetic route keeping in view the structural requirement of pharmacophore and evaluated for anticonvulsant activity and CNS activities. After intraperitoneal injection to mice, some synthesized derivatives were examined in the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazol (scPTZ) induced seizure and neurotoxicity screens. Those found potent were also evaluated for behavioural impairment and depression activity. Among the compound tested, 5 eIX showed protection from seizures in both the animal models at dose level of 30 mg/kg while 5 bII &5 cII showed protection against scPTZ model at same dose level. Some titled compounds exhibited lesser CNS depression and neurotoxicity compared to clinically effective drug.
Kaushik
Darpan
D
Medicinal Chemistry Division, F/O Pharmacy, Jamia Hamdard, New Delhi 125055, India. darpkaush@yahoo.com
Khan
Suroor Ahmad
SA
Chawla
Gita
G
D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity; D001522:Behavior, Animal / Q000187:drug effects; D015195:Drug Design; D004597:Electroshock / Q000009:adverse effects; D008297:Male; D051379:Mice; D009420:Nervous System / Q000187:drug effects; D010433:Pentylenetetrazole / Q000494:pharmacology; D012640:Seizures / Q000139:chemically induced / Q000188:drug therapy; D014227:Triazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity
D000927:Anticonvulsants; D014227:Triazines; D010433:Pentylenetetrazole