Your browser doesn't support javascript.
loading
Design, synthesis and biological evaluation of novel desloratadine derivatives with anti-inflammatory and H1 antagonize activities.
Li, Feng; Xu, Qinlong; Zhu, Qihua; Chu, Zhaoxing; Lin, Gaofeng; Mo, Jiajia; Zhao, Yan; Li, Jiaming; He, Guangwei; Xu, Yungen.
Affiliation
  • Li F; Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China; Hefei Institute of Pharmaceutical Industry Co., Ltd., Hefei 230088, China.
  • Xu Q; Hefei Institute of Pharmaceutical Industry Co., Ltd., Hefei 230088, China; Anhui University of Chinese Medicine, Hefei 230031, China.
  • Zhu Q; Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China; Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 21009, China.
  • Chu Z; Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China; Hefei Institute of Pharmaceutical Industry Co., Ltd., Hefei 230088, China.
  • Lin G; Hefei Institute of Pharmaceutical Industry Co., Ltd., Hefei 230088, China.
  • Mo J; Hefei Institute of Pharmaceutical Industry Co., Ltd., Hefei 230088, China.
  • Zhao Y; Hefei Institute of Pharmaceutical Industry Co., Ltd., Hefei 230088, China.
  • Li J; Anhui University of Chinese Medicine, Hefei 230031, China.
  • He G; Hefei Institute of Pharmaceutical Industry Co., Ltd., Hefei 230088, China.
  • Xu Y; Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China; Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 21009, China. Electronic address: xu_yungen@hotmail.com.
Bioorg Med Chem Lett ; 29(24): 126712, 2019 12 15.
Article in En | MEDLINE | ID: mdl-31679973
ABSTRACT
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.
Subject(s)
Key words
Fulltext
Add to My VHL
Print
XML
PubMed Links
Search on Google

Full text: 1 Database: MEDLINE Main subject: Loratadine / Histamine H1 Antagonists / Anti-Inflammatory Agents Limits: Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2019 Type: Article Affiliation country: China
Fulltext
Add to My VHL
Print
XML
PubMed Links
Search on Google

Full text: 1 Database: MEDLINE Main subject: Loratadine / Histamine H1 Antagonists / Anti-Inflammatory Agents Limits: Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2019 Type: Article Affiliation country: China