Dimmock J R, Vashishtha S C, Stables J P
College of Pharmacy and Nutrition, University of Saskatchewan, Saskatoon, Saskatchewan, Canada.
Eur J Med Chem. 2000 Feb;35(2):241-8. doi: 10.1016/s0223-5234(00)00123-9.
Various acetylhydrazones, oxamoylhydrazones and semicarbazones were prepared as candidate anticonvulsants with a view to examining the viability of a putative binding site hypothesis. Atomic charge calculations were undertaken to determine the hydrogen bonding capacities of various molecules. The biological results obtained revealed that in general the acetylhydrazones and semicarbazones afforded good protection against convulsions while the oxamoylhydrazones were significantly less active. These data suggest that terminal electron-donating groups enhanced the hydrogen bonding capabilities and anticonvulsant properties of these molecules.
制备了各种乙酰腙、草酰肼腙和氨基脲，作为候选抗惊厥剂，以检验一种假定的结合位点假说的可行性。进行了原子电荷计算，以确定各种分子的氢键结合能力。所获得的生物学结果表明，一般来说，乙酰腙和氨基脲能提供良好的抗惊厥保护作用，而草酰肼腙的活性则明显较低。这些数据表明，末端供电子基团增强了这些分子的氢键结合能力和抗惊厥特性。
