论文部分内容阅读
前文曾报道,在研究桂皮酰胺类化合物构效关系的基础上设计合成的3-烷基-6-苯基-4(3H)-嘧啶酮类化合物多数有抗惊活性,但比预期的弱,其中苯环不带取代基的6-本基-4(3H)-嘧啶酮(Ⅰ)抗惊作用较强(MES ED_(50) 91·7 mg/kg)。为找到抗惊作用更强的化合物,我们设想将Ⅰ环上4位氧原子改变成氮原子从而得到4-氨基-6-苯基嘧啶类化合物(Ⅱ),仍保持苯环与嘧啶环共轭系统不变,再以不同烃基取代氨基氮上的氢原子,可得到脂溶性不同,局部空间
It has been previously reported that most of the 3-alkyl-6-phenyl-4 (3H) -pyrimidinones designed and synthesized on the basis of studying the structure-activity relationship of cinnamide compounds have anticonvulsant activity but are weaker than expected, The 6-benzyloxy-4 (3H) -pyrimidinone (Ⅰ) with no substituent on the benzene ring showed strong anti-shock activity (MES ED_ (50) 91.7 mg / kg). In order to find out the more anti-antiviral compounds, we envisaged that the 4-amino-6-phenylpyrimidine compound (II) was obtained by changing the oxygen atom of the 4th ring in the Ⅰ ring to a nitrogen atom, while still maintaining the conjugation of the benzene ring and the pyrimidine ring System unchanged, and then replace the different hydrogen atoms on the amino nitrogen, you can get different fat-soluble, local space