Anticonvulsant and sedative-hypnotic activities of N-substituted isatin semicarbazones.
A series of N-methyl/acetyl, 5-(un)-substituted isatin-3-semicarbazones were screened for anticonvulsant and sedative-hypnotic activities. The results revealed that protection was obtained in all the screens i.e., MES, scPTZ, and scSTY. Compounds 2, 4, 6, 10 but not 1 and 3 showed low neurotoxicity when compared to clinically used drugs. Compounds 5, 7, 8 and 9 were completely non-toxic. Compound 6 showed good activity in the rat oral MES screen. Among all the compounds, 3 and 6 emerged as the most active compounds as indicated by the protection they exhibit in MES, scSTY, and scPTZ screens. All the compounds showed significant sedativehypnotic activity.
Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi, India. snpande@banaras.ernet.in
Surendra N
SN
Pandeya
Sivakumar
S
Smitha
James P
JP
Stables
D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D003292:Convulsants; D006993:Hypnotics and Sedatives / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D007510:Isatin / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D010433:Pentylenetetrazole; D051381:Rats; D017207:Rats, Sprague-Dawley; D012640:Seizures / Q000139:chemically induced / Q000517:prevention & control; D012664:Semicarbazones / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D013055:Spectrophotometry, Infrared
D000927:Anticonvulsants; D003292:Convulsants; D006993:Hypnotics and Sedatives; D012664:Semicarbazones; D007510:Isatin; D010433:Pentylenetetrazole