Cates L A, Li V S, Yakshe C C, Fadeyi M O, Andree T H, Karbon E W, Enna S J
J Med Chem. 1984 May;27(5):654-9. doi: 10.1021/jm00371a017.
A series of phosphorus compounds, designed as analogues of gamma-aminobutyric acid (GABA) in that they possess a P = O moiety separated by three atoms from an amino or acetamido group, was synthesized and tested by using in vitro GABAA and GABAB receptor binding, GABA uptake assays, and was examined for anticonvulsant activity. Weak GABAB receptor affinity was noted for one agent, whereas six compounds displayed moderate to high potencies as inhibitors of electroshock- and pentylenetetrazol-induced seizures. The best anticonvulsant effect was found with the (m-aminophenyl) phosphinic acid compounds, with members of this class selected for further study.
设计了一系列磷化合物，它们是γ-氨基丁酸（GABA）的类似物，因为它们具有一个与氨基或乙酰氨基被三个原子隔开的P = O部分。通过体外GABAA和GABAB受体结合、GABA摄取试验对其进行了合成和测试，并检测了其抗惊厥活性。其中一种化合物表现出较弱的GABAB受体亲和力，而六种化合物作为电休克和戊四氮诱导癫痫发作的抑制剂表现出中度至高效力。（间氨基苯基）次膦酸化合物具有最佳的抗惊厥效果，因此选择该类成员进行进一步研究。
