Anticonvulsant and neurotoxicity evaluation of some 6-chlorobenzothiazolyl-2-thiosemicarbazones.
Ten 6-chlorobenzothiazolyl-2-thiosemicarbazones were synthesised and screened for anticonvulsant and neurotoxic properties. Most of the compounds showed anticonvulsant activity against both maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole screens. Eight compounds have shown good protection in the rat p.o. MES test at 30 mg kg(-1). Compound 1 [4-(6-chlorobenzothiazol-2-yl)-1-(3-isatinimino)thiosemicarbazone] emerged as the most promising one with an ED(50) of 17.86 and 6.07 mg kg(-1) in mice i.p. and rat p.o., respectively. Compound 1 showed a weak ability to block the expression of fully kindled seizures.
Yogeeswari
Perumal
P
Medicinal Chemistry Research Laboratory, Pharmacy Group, Birla Institute of Technology & Science, Pilani 333 031, India. pyogie_2000@rediffmail.com
Sriram
Dharmarajan
D
Sunil Jit
Logantha Ramamoorthy Jeewanlal
LR
Kumar
Sathiyanesan Sathish
SS
Stables
James P
JP
D000679:Amygdala / Q000187:drug effects / Q000502:physiology; D000818:Animals; D000927:Anticonvulsants / Q000008:administration & dosage / Q000138:chemical synthesis / Q000627:therapeutic use* / Q000633:toxicity*; D004353:Drug Evaluation, Preclinical; D004597:Electroshock; D007696:Kindling, Neurologic / Q000187:drug effects; D051379:Mice; D015394:Molecular Structure; D051381:Rats; D012640:Seizures / Q000139:chemically induced / Q000188:drug therapy*; D013882:Thiosemicarbazones / Q000008:administration & dosage / Q000138:chemical synthesis / Q000627:therapeutic use* / Q000633:toxicity*
D000927:Anticonvulsants; D013882:Thiosemicarbazones