Cyclization of the semicarbazone template of aryl semicarbazones: synthesis and anticonvulsant activity of 4,5-diphenyl-2H-1,2,4-triazol-3(4H)-one.
A new series of 4,5-diphenyl-2H-1,2,4-triazol-3(4H)-one were synthesized to study the effect of cyclization of the semicarbazone moiety of aryl semicarbazones on the anticonvulsant activity. Structures of the synthesized compounds were confirmed by the use of their spectral data besides elemental analysis. All compounds were evaluated for their anticonvulsant activity in four animal models of seizures, viz. maximal electroshock seizure (MES), subcutaneous pentylenetetrazole (scPTZ), subcutaneous strychnine (scSTY), and subcutaneous picrotoxin (scPIC)-induced seizure threshold tests. The compounds were also evaluated for neurotoxicity. Compounds 4, 9, 14-19 exhibited anticonvulsant activity in all the four animal models of seizure.
Medicinal Chemistry Research Laboratory, Pharmacy Group, Birla Institute of Technology and Science, 333031 Pilani, India
M
M
Shalini
P
P
Yogeeswari
D
D
Sriram
J P
JP
Stables
D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D004195:Disease Models, Animal; D004597:Electroshock; D008297:Male; D051379:Mice; D010433:Pentylenetetrazole; D010852:Picrotoxin; D051381:Rats; D017207:Rats, Sprague-Dawley; D012640:Seizures / Q000188:drug therapy*; D012664:Semicarbazones / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D013329:Structure-Activity Relationship; D013331:Strychnine; D018675:Toxicity Tests
D000927:Anticonvulsants; D010433:Pentylenetetrazole; D010852:Picrotoxin; D012664:Semicarbazones; D013331:Strychnine