Anticonvulsant and neurotoxicity evaluation of some 6-substituted benzothiazolyl-2-thiosemicarbazones.
Various 6-substituted benzothiazolyl-2-thiosemicarbazones were synthesized and screened for anticonvulsant activity in maximal electroshock induced seizure (MES) and subcutaneous pentylenetetrazole (scPTZ) induced seizure models in mice. The neurotoxicity was assessed using the rotorod method. The 6-methyl benzothiazolyl-2-thiosemicarbazones showed anticonvulsant activity in both mice i.p. and rat oral MES screen. The 6-nitro benzothiazolyl thiosemicarbazone derivative 1a emerged as the most promising one with anti-MES activity in mice i.p., rat i.p. and rat p.o. evaluations. All the compounds exhibited lesser or no neurotoxicity compared to phenytoin. The isatinimino derivatives had shown better activity when compared to the benzylidene or acetophenone derivatives.
Yogeeswari
P
P
Medicinal Chemistry Research Laboratory, Pharmacy Group, Birla Institute of Technology & Science, Pilani-333031, India. pyogee@bits-pilani.ac.in
Sriram
D
D
Mehta
S
S
Nigam
D
D
Kumar
M Mohan
MM
Murugesan
S
S
Stables
J P
JP
D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis / Q000627:therapeutic use / Q000633:toxicity*; D003292:Convulsants / Q000633:toxicity; D004353:Drug Evaluation, Preclinical; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D010433:Pentylenetetrazole / Q000633:toxicity; D051381:Rats; D017207:Rats, Sprague-Dawley; D012640:Seizures / Q000139:chemically induced / Q000188:drug therapy*; D013329:Structure-Activity Relationship; D013882:Thiosemicarbazones / Q000138:chemical synthesis / Q000627:therapeutic use / Q000633:toxicity*
D000927:Anticonvulsants; D003292:Convulsants; D013882:Thiosemicarbazones; D010433:Pentylenetetrazole