Synthesis and anticonvulsant activities of 4-N-substituted arylsemicarbazones.
A series of 4-N-substituted arylsemicarbazones with increased lipophilicity were synthesized and evaluated for anticonvulsant activity. The compounds provided significant protection against maximal electroshock induced seizures (MES) and seizures indicated by sc pentetrazole administration (sc PTZ) at 300 mg/kg after 0.5 h. The compounds 8 and 4 were active in MES and sc PTZ indicated seizure. The study has shown that introduction of alkyl (ethyl) at the terminal amino group and alkoxy (methoxy) moiety at the distal aryl ring led to increased activity and decreased toxicity.
Pandeya
Surendra N
SN
University of Pharmaceutics, Institute of Technology, Banams Hindu University, Varanasi--221005, India. snpandeya@rediffmail.com
Kohli
Sonia
S
Siddique
Nadeem
N
Stables
James P
JP
D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004597:Electroshock; D006993:Hypnotics and Sedatives / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D051379:Mice; D008956:Models, Chemical; D015394:Molecular Structure; D009043:Motor Activity / Q000187:drug effects; D010433:Pentylenetetrazole; D012640:Seizures / Q000209:etiology / Q000517:prevention & control; D012664:Semicarbazones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D012890:Sleep / Q000187:drug effects; D013329:Structure-Activity Relationship; D013997:Time Factors
D000927:Anticonvulsants; D006993:Hypnotics and Sedatives; D012664:Semicarbazones; D010433:Pentylenetetrazole