某些6-氯苯并噻唑基-2-硫代氨基脲的抗惊厥和神经毒性评估
Anticonvulsant and neurotoxicity evaluation of some 6-chlorobenzothiazolyl-2-thiosemicarbazones.
作者信息
Yogeeswari Perumal, Sriram Dharmarajan, Sunil Jit Logantha Ramamoorthy Jeewanlal, Kumar Sathiyanesan Sathish, Stables James P
机构信息
Medicinal Chemistry Research Laboratory, Pharmacy Group, Birla Institute of Technology & Science, Pilani 333 031, India.
出版信息
Eur J Med Chem. 2002 Mar;37(3):231-6. doi: 10.1016/s0223-5234(02)01338-7.
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.
合成了10种6-氯苯并噻唑基-2-硫代氨基脲，并对其抗惊厥和神经毒性进行了筛选。大多数化合物对最大电休克惊厥（MES）和皮下注射戊四氮筛选均显示出抗惊厥活性。8种化合物在大鼠口服MES试验中，剂量为30mg/kg时显示出良好的保护作用。化合物1 [4-(6-氯苯并噻唑-2-基)-1-(3-异吲哚酮亚氨基)硫代氨基脲]是最有前景的一种，在小鼠腹腔注射和大鼠口服时的半数有效剂量（ED50）分别为17.86和6.07mg/kg。化合物1阻断完全点燃惊厥表达的能力较弱。
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