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本文在前报的基础上,设计和合成了4-芳杂环取代的氨甲基酚衍生物28个。初步药理试验表明,多数显示不同程度的抗炎活性。用CNDO/2法计算所得数据提示,该类化合物分子中的氨甲基氮和酚羟基氧与受体正电荷中心的结合,可能对抗炎活性起着重要作用。
In this paper, based on the previous report, the design and synthesis of 4 - arylheterocyclic substituted aminomethyl phenol derivatives 28. Preliminary pharmacological tests show that most show varying degrees of anti-inflammatory activity. The data calculated by CNDO / 2 method suggest that the combination of aminomethyl nitrogen and phenolic hydroxyl oxygen in the molecules of these compounds with the positive charge center of the receptor may play an important role in anti-inflammatory activity.