3-烃基-4-苯基双环硫（氧）化磷酸酯的合成研究

研究双环硫化磷酸酯类化合物在大鼠及家蝇神经节结合部位有抗GABA（γ-氨基丁酸）作用，并对其进行了放射性配体与大鼠及家蝇GABA受体的结合活性测定，研究其抑制活性和生物选择性. 以2-苯基丙二酸二乙酯为原料，经酰化、还原及环合3步反应得到10个3-烃基-4-苯基双环笼状磷酸酯类化合物，所有化合物均通过1H NMR和MS进行了结构确认，采用放射性配体—受体结合试验，测定了10个化合物抑制［3H］EBOB（4’-乙炔基-4-正丙基原苯甲酸酯）与家蝇及大鼠GABA受体的结合活性，结果表明部分化合物在10-5 mol/L具有较好的抑制活性，且在大鼠与家蝇GABA受体之间有一定的选择性.

Synthesis of 3-alkyl-4-phenyl Bicyclophosphorothionate

The anti-γ-aminobutyric acid （GABA） effects of the bicyclophosphorothionate compounds on the ganglion sites of rats and houseflies were explored， and the binding activities between the radioligands and GABA receptor were tested to study the inhibitory activities and biological selectivity of the bicyclophosphorothionate compounds. Ten 3-hydroxy-4-phenyl-bicyclophosphate compounds were synthesized by using 2-phenyl-diethylmalonate as a starting material via acylation， reduction and cyclization， and their structures were determined by 1H nuclear magnetic resonance spectrocopy and mass spectrometry. In addition， the radioligand binding assay was performed to evaluate the potencies of the bicyclophosphorothionate compounds to inhibit the binding of ［3H］ ethynylbicycloorthobenzoate to GABA receptors of rats and houseflies， and the results show that these compounds have relatively high binding activities and certain selectivity to GABA receptors of rats and houseflies at the concentration of 10-5 mol/L.