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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Design and synthesis of bioactive adamantanaminoalcohols and adamantanamines.
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Design and synthesis of bioactive adamantanaminoalcohols and adamantanamines.

机译：生物活性亚丹丹氨基醇和吲哚美沙胺的设计与合成。

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摘要

Adamantanamines 16, 18, 21, 24, 27, 28, 30, 32, 35, 36, 37, 40, 46 and 48 were synthesized and tested for anti-influenza A virus and trypanocidal activity. The stereoelectronic requirements for optimal antiviral and trypanocidal potency were investigated. The effect of introducing a hydroxyl group close to the amino group on this class of compounds was examined for the first time. Aminoalcohol 24 proved to be the most active of the compounds tested against influenza A virus, being 6-fold more active than amantadine, equipotent to rimantadine and 26-fold more potent than ribavirin. Aminoalcohols 36 and 37 were found to have considerable activity against bloodstream forms of the African trypanosome, Trypanosoma brucei, being almost 10 times more potent than rimantadine.
机译：合成并测试抗流感病毒和锥体灭绝活性的亚氨基甲胺胺16,18,21,24,27,28,30,32,35,26,37,28,40,46和48。 研究了最佳抗病毒和胰蛋白酶效力的立体电子要求。 第一次检测将近于氨基靠近氨基的羟基的效果。 氨基醇24被证明是对受甲型病毒测试的化合物中最活跃的，比氨基氨基更活跃6倍，使rymantadine等待，比利巴韦林更有效。 发现氨基醇36和37对非洲锥虫瘤的血液形式具有相当大的活动，葡萄干瘤Brucei的血液瘤细胞瘤，比rimantadine更有效的近10倍。

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