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Ⅰ,以2,6—双(二甲胺甲基)—4—正十二烷基苯酚二盐酸为先导物,设计并合成了十四个酚Mannich碱。药理试验表明,在二元酚Mannich碱中,化合物的疏水性对抗沙眼衣原体活性有很大影响。疏水性略小于先导物时,化合物的抗沙眼衣原体活性显著增强,其活性XVI为先导物的四倍,XIV、XV为先导物的八倍。Ⅱ,以2,6—双(二甲胺甲基)—4—正十二烷基苯酚二盐酸盐为先导物,根据拼合原理设计了1—(4＇—羟基苯基)正十二烷酮—1的酚Mannich碱(Ⅱ)及其三个衍生物,然后合成之。在这些化合物中,化合物Ⅱ的抗沙眼衣原体活性最强,约为先导物活性的二倍。
Ⅰ. Fourteen phenolic Mannich bases were designed and synthesized with 2,6-bis (dimethylaminomethyl) -4-n-dodecylphenol dihydrochloride as the lead. Pharmacological tests show that the hydrophobicity of the compound in the dihydric phenol Mannich base greatly affects the activity of Chlamydia trachomatis. When the hydrophobicity is slightly less than that of the lead, the activity of the compounds against Chlamydia trachomatis is significantly enhanced, with the activity of XVI being four times that of the lead and XIV and XV being eight times the lead. Ⅱ, using 2,6-bis (dimethylaminomethyl) -4-n-dodecylphenol dihydrochloride as the leader, according to the principle of combining design 1- (4’-hydroxyphenyl) The alkanone-1-containing Mannich base (II) and its three derivatives are then synthesized. Of these compounds, compound II was the most active against C. trachomatis, about twice as active as the leader.