Evaluation of semicarbazones for anticonvulsant and sedative-hypnotic properties.
A series of semicarbazones and thiosemicarbazones were synthesized and evaluated for anti-convulsant activity. Some compounds provided significant protection against Maximal Electroshock (MES) and subcutaneous strychnine induced seizures. Compound 1 was the most active in the series with activity in a dose of 30 mg/kg in the strychnine seizure pattern test and an ED50 of 10 mg/kg in the MES test. Hence it could serve as a prototype molecule for future development. Also compounds with a p-nitrophenyl substitution in place of the amino hydrogen of semicarbazone moiety showed activity in a dose of 30 mg/kg and an ED50 of 83 mg/kg in the MES test.
Pandeya
S N
SN
Department of Pharmaceutics, Banaras Hindu University, Varanasi, India.
Aggarwal
N
N
Jain
J S
JS
D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D003292:Convulsants / Q000633:toxicity; D004597:Electroshock; D006993:Hypnotics and Sedatives / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D004856:Postural Balance / Q000187:drug effects; D012640:Seizures / Q000139:chemically induced / Q000517:prevention & control; D012664:Semicarbazones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D012890:Sleep / Q000187:drug effects; D013055:Spectrophotometry, Infrared; D013329:Structure-Activity Relationship; D013331:Strychnine / Q000037:antagonists & inhibitors / Q000633:toxicity; D013997:Time Factors
D000927:Anticonvulsants; D003292:Convulsants; D006993:Hypnotics and Sedatives; D012664:Semicarbazones; D013331:Strychnine