Design, synthesis and biological evaluation of novel desloratadine derivatives with anti-inflammatory and H1 antagonize activities.
Design, synthesis and biological evaluation of novel desloratadine derivatives with anti-inflammatory and H1 antagonize activities.
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DOI：
10.1016/j.bmcl.2019.126712
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发表时间：
2019-10
影响因子：
2.7
通讯作者：
Feng Li;Qinlong Xu;Qihua Zhu;Zhaoxing Chu;Gaofeng Lin;Jiajia Mo;Yan Zhao;Jiaming Li;Guangwei He;Yungen Xu
中科院分区：
文献类型：
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作者：
Feng Li;Qinlong Xu;Qihua Zhu;Zhaoxing Chu;Gaofeng Lin;Jiajia Mo;Yan Zhao;Jiaming Li;Guangwei He;Yungen Xu
为了提高地氯雷他定的抗炎活性，我们设计并合成了一系列新的地氯雷他定衍生物。对所有化合物的抗炎和抗h1活性进行了评价。其中化合物2表现出最强的抗h1和抗炎活性。它还表现出良好的药代动力学特征和低毒性。这些结果表明化合物2是一种值得进一步研究的新型抗过敏药物。
To improve the anti-inflammatory activity of desloratadine, we designed and synthesized a series of novel desloratadine derivatives. All compounds were evaluated for their anti-inflammatory and H1antagonistic activities. Among them, compound2cshowed the strongest H1antagonistic and anti-inflammatory activity. It also exhibited promising pharmacokinetic profiles and low toxicity. All these results suggest that compound2cas a novel anti-allergic agent is worthy of further investigation.