Andrews P R, Jones G P, Lodge D
Eur J Pharmacol. 1979 Apr 15;55(2):115-20. doi: 10.1016/0014-2999(79)90382-0.
Barbiturates derived by minor structural changes to the butenyl sidechain of the convulsant 5-ethyl-5-(3'-methyl-but-2'-enyl)-barbituric acid are almost devoid of convulsant activity, but all have anaesthetic and anticonvulsant effects. Anticonvulsant activity is also observed in the convulsant barbiturate. Increased lipophilic character does not increase anaesthetic potency, only speed of onset, and anticonvulsant activity is reduced in the more lipophilic compounds. The stereochemistry at the 3'-position of the sidechain is vitally important to convulsant activity, and also influences anticonvulsant potency.
通过对惊厥性5-乙基-5-(3'-甲基-丁-2'-烯基)-巴比妥酸的丁烯基侧链进行微小结构变化而得到的巴比妥类药物几乎没有惊厥活性，但都具有麻醉和抗惊厥作用。在惊厥性巴比妥酸盐中也观察到抗惊厥活性。亲脂性增加并不会提高麻醉效力，只会加快起效速度，并且在亲脂性更强的化合物中抗惊厥活性会降低。侧链3'-位的立体化学对惊厥活性至关重要，并且也会影响抗惊厥效力。
