Dimmock J R, Brenner J M, Phillips O A
College of Pharmacy, University of Saskatchewan, Saskatoon, Canada.
Pharmazie. 1987 Jun;42(6):376-8.
Benzaldehyde benzenesulphonamide was shown to have comparable anticonvulsant activity to valproic acid in the maximal electroshock seizure test. Molecular modification of this compound was developed principally to explore whether a correlation between planarity and anticonvulsant activity could be discerned. The interplanar angle (theta) between an aryl ring and the adjacent azomethine group of some representative compounds was measured by electronic absorption spectroscopy. However, the structural alterations of benzaldehyde benzenesulphonamide undertaken in this work led to compounds bereft of anticonvulsant activity.
在最大电休克惊厥试验中,苯甲醛苯磺酰胺显示出与丙戊酸相当的抗惊厥活性。对该化合物进行分子修饰主要是为了探究是否能发现平面性与抗惊厥活性之间的相关性。通过电子吸收光谱法测量了一些代表性化合物中芳环与相邻偶氮甲碱基团之间的平面夹角(θ)。然而,这项工作中对苯甲醛苯磺酰胺进行的结构改变导致得到的化合物失去了抗惊厥活性。