Srivastava K, Pandeya S N
Department of Pharmaceutics, Banaras Hindu University, Varanasi, India.
Boll Chim Farm. 1992 Sep;131(8):313-7.
A series of 4-aryl-3-arylamino-5-imino-1,2,4-thiadiazolidines (1a-k) and 4-aryl-3-arylamino-5-oxo-1,2,4-thiadiazolidines (2a-k) were evaluated for their anticonvulsant and analgesic activity. Substitution of p-methoxy group (1g) in the aryl ring resulted in more active compounds than the standard drug phenytoin in the MES test, whereas in the chemoshock test the compounds were found inactive. In the analgesic test most of the compounds exhibited analgesic activity with particular reference to p-Br (1k) and m-Cl (1i) substitutions which were most potent in this series.
对一系列4-芳基-3-芳氨基-5-亚氨基-1,2,4-噻二唑烷(1a-k)和4-芳基-3-芳氨基-5-氧代-1,2,4-噻二唑烷(2a-k)进行了抗惊厥和镇痛活性评估。芳环中对甲氧基(1g)的取代产生了比标准药物苯妥英在最大电休克(MES)试验中更具活性的化合物,而在化学性惊厥试验中发现这些化合物无活性。在镇痛试验中,大多数化合物表现出镇痛活性,特别是对溴(1k)和间氯(1i)取代的化合物在该系列中最为有效。