Design, synthesis and biological evaluation of novel desloratadine derivatives with anti-inflammatory and H1 antagonize activities

• Published in: Bioorganic & medicinal chemistry letters Vol. 29; no. 24; p. 126712
• Main Authors: Li, Feng, Xu, Qinlong, Zhu, Qihua, Chu, Zhaoxing, Lin, Gaofeng, Mo, Jiajia, Zhao, Yan, Li, Jiaming, He, Guangwei, Xu, Yungen
• Format: Journal Article
• Language: English
• Published: Elsevier Ltd 15-12-2019
• Subjects: Anti-allergic; Anti-inflammatory; Desloratadine; H1 antagonize; Anti-allergic; H1 antagonize; Anti-inflammatory; Desloratadine
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2019.126712

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 H1 antagonistic activities. Among them, compound 2c showed the strongest H1 antagonistic and anti-inflammatory activity. It also exhibited promising pharmacokinetic profiles and low toxicity. All these results suggest that compound 2c as a novel anti-allergic agent is worthy of further investigation.
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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 H1 antagonistic activities. Among them, compound 2c showed the strongest H1 antagonistic and anti-inflammatory activity. It also exhibited promising pharmacokinetic profiles and low toxicity. All these results suggest that compound 2c as a novel anti-allergic agent is worthy of further investigation.