Synthesis of aryl semicarbazones as potential anticonvulsant agents.
A series of 4-ethoxyphenyl semicarbazones (1-10) have been synthesized using an appropriate synthetic route and characterized by elemental analyses and spectral data. The anticonvulsant activity of all the synthesized compounds was evaluated against maximal electroshock induced seizures (MES) and subcutaneous pentylenetetrazole (scPTZ) induced seizure models in mice. The neurotoxicity was assessed using the rotorod method. All the test compounds were administered at doses of 30, 100, and 300 mg/kg body weight and the anticonvulsant activity was noted at 0.5 and 4 h time intervals after the drug administration. Among the compounds tested, compounds except 3, 4 and 10 showed protection from seizures in both the animal models. Compounds 6 and 8 were found to increase gamma-aminobutyric acid (GABA) levels in the medulla oblongata region of the rat brain.
Yogeeswari
P
P
Medicinal Chemistry Research Laboratory, Pharmacy Group, Birla Institute of Technology and Science, Pilani 333031, India. pyogee@bits-pilani.ac.in
Sriram
D
D
Veena
V
V
Kavya
R
R
Rakhra
K
K
Ragavendran
J Vaigunda
JV
Mehta
S
S
Thirumurugan
R
R
Stables
J P
JP
D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use*; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D004597:Electroshock / Q000379:methods; D008297:Male; D051379:Mice; D051381:Rats; D017207:Rats, Sprague-Dawley; D012640:Seizures / Q000188:drug therapy / Q000378:metabolism; D012664:Semicarbazones / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use*
D000927:Anticonvulsants; D012664:Semicarbazones