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从苔藓虫Zoobotryon pellucidum中提取的2,5,6-三溴-1-甲基芦竹碱(TBG)能较好地抑制海洋生物藤壶的附着.为提高该类化合物在防污涂料中的复配性能,合成了4个新型的不同卤素取代和N-取代且具有较好亲脂性能的TBG类似物.通过1H NMR,13C NMR,IR和元素分析对目标化合物6a～6d进行了结构表征.生物实验结果表明,化合物5～6对海藻Nitzschia closterium均具有较好的生长抑制活性,其中以亲脂性较强的6b和6d抑制作用最为显著,LC50分别可达1.33μg/mL和1.06μg/mL.对化合物的定量构效关系进行了初步探讨.
Trimethoprim (TBG) extracted from the bryozoan Zoobotryon pellucidum can inhibit the attachment of marine barnacles better.In order to improve the antifouling properties of these compounds 4 novel TBG analogs with different halogen substitutions and N-substitution and good lipophilicity were synthesized.The structures of target compounds 6a ~ 6d were characterized by 1H NMR, 13C NMR, IR and elemental analysis The results of biological experiments showed that compounds 5 to 6 had good growth inhibitory activity against the seaweed Nitzschia closterium, of which the lipophilic activity of 6b and 6d was the most significant, with LC50 of 1.33μg / mL and 1.06μg / mL. The quantitative structure-activity relationship of the compounds was discussed.