Rankin G O, Riley T N, Murphy J C
J Med Chem. 1978 May;21(5):460-4. doi: 10.1021/jm00203a010.
A series of substituted 3-aryl- and hydroxy-3-aryloctahydropyrido[2,1-c][1,4]oxazines has been synthesized for purposes of investigating potentially useful CNS pharmacological actions of this novel heterocyclic system. The preferred conformation of the bicyclic system of the parent compounds, 1 and 2, has been shown to be trans with equatorial orientation of the 3-phenyl substituent in each compound. The various substituted aryl analogues of this series are depressants of motor activity in mice, and certain analogues exhibit significant anticonvulsant and appetite suppressant activity in test animals.
为了研究这种新型杂环体系潜在的有用的中枢神经系统药理作用，已合成了一系列取代的3-芳基-和羟基-3-芳基八氢吡啶并[2,1-c][1,4]恶嗪。母体化合物1和2的双环体系的优选构象已显示为反式，每个化合物中3-苯基取代基呈平伏取向。该系列的各种取代芳基类似物是小鼠运动活性的抑制剂，某些类似物在试验动物中表现出显著的抗惊厥和食欲抑制活性。
