一些取代香豆素作为抗惊厥剂的合成及初步评价
Synthesis and preliminary evaluation of some substituted coumarins as anticonvulsant agents.
作者信息
Amin Kamelia M, Rahman Doaa E Abdel, Al-Eryani Yasmin A
机构信息
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Cairo 11562, Egypt.
出版信息
Bioorg Med Chem. 2008 May 15;16(10):5377-88. doi: 10.1016/j.bmc.2008.04.021. Epub 2008 Apr 15.
Some new substituted coumarinylthiazolines, coumarinylthiazolidin-4-ones, and substituted chromenothiazoles were synthesized and evaluated for anticonvulsant activity. Some selected compounds were assayed against seizures induced by pentylenetetrazole (PTZ) and strychnine in mice. Compounds 3b, 6b, and 7b were the most active of the series against PTZ induced seizures. Compound 7b provided anticonvulsant activity (PD(50)=95mg/kg, ip) at a dose 200mg/kg compared to phenobarbital (PD(50)=16mg/kg, ip) at a dose 30mg/kg (90% protection). No clear correlation was observed between the antiepileptic activity and molecular lipophilicity descriptors of the tested compounds.
合成了一些新型取代香豆素基噻唑啉、香豆素基噻唑烷-4-酮和取代色烯并噻唑，并对其抗惊厥活性进行了评估。对一些选定的化合物进行了抗戊四氮（PTZ）和士的宁诱导小鼠惊厥的测定。化合物3b、6b和7b是该系列中对PTZ诱导惊厥活性最高的。与苯巴比妥（腹腔注射半数有效量PD(50)=16mg/kg，剂量30mg/kg，90%保护率）相比，化合物7b在剂量200mg/kg时提供抗惊厥活性（腹腔注射半数有效量PD(50)=95mg/kg）。在所测试化合物的抗癫痫活性与分子亲脂性描述符之间未观察到明显的相关性。
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