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.
Pandeya
Surendra N
SN
Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi, India. snpande@banaras.ernet.in
Smitha
Sivakumar
S
Stables
James P
JP
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