Lee C H, Kohn H
Department of Chemistry, University of Houston, TX 77204-5641.
J Pharm Sci. 1990 Aug;79(8):716-8. doi: 10.1002/jps.2600790813.
Selectively substituted 3-oxo-4-substituted 1,2,5-thiadiazolidine 1,1-dioxides (2, four examples), and 3-imino-4-substituted 1,2,5-thiadiazolidine 1,1-dioxides (3, eight examples) have been evaluated in the maximal electroshock seizure (MES), subcutaneous pentylenetetrazole seizure threshold (scMet), and rotorod (Tox) tests. These compounds can be considered as sulfonyl analogues of hydantoins (1). In those cases where comparison between 1 and 2 (or 1 and 3) was possible, replacement of the central carbonyl group in 1 by a sulfonyl moiety led to a significant reduction or abolition of the anticonvulsant activity.
已在最大电休克惊厥（MES）、皮下注射戊四氮惊厥阈值（scMet）和转棒试验（Tox）中对选择性取代的3-氧代-4-取代-1,2,5-噻二唑烷1,1-二氧化物（2，4个实例）和3-亚氨基-4-取代-1,2,5-噻二唑烷1,1-二氧化物（3，8个实例）进行了评估。这些化合物可被视为乙内酰脲（1）的磺酰类似物。在能够对1和2（或1和3）进行比较的情况下，将1中的中心羰基用磺酰部分取代会导致抗惊厥活性显著降低或丧失。
