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Design, synthesis and biological activity evaluation of desloratadine analogues as H1 receptor antagonists.

Author: CaoXiao-Hui, ChenBo, ChenLi-Gong, LinYan, SimaLi-Feng, WangDong-Hua, WangYue

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Overview

A series of N-substituted desloratadine analogues were synthesized and tested for antihistamine activity, leading to the identification of compound 10, (1S,4S)-4-chlorocyclohexyl desloratadine, with high activity and a good safety profile.
Paper Details　
Original Abstract of the Article :
A series of N-substituted desloratadine analogues were designed and synthesized. They were tested for H1 antihistamine activity by inhibiting histamine-induced contraction of isolated ileum muscles of guinea-pigs in vitro and inhibiting histamine-induced asthmatic reaction in guinea-pigs in vivo. Al...See full text at original site
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引用元：
https://doi.org/10.1016/j.bmc.2013.05.004

データ提供：米国国立医学図書館（NLM）

Desloratadine Analogues: Exploring New Antihistamine Candidates

The search for effective and safe antihistamines is a continuous pursuit, much like a desert explorer searching for a new oasis. This study explores the potential of desloratadine analogues as H1 receptor antagonists, seeking to develop improved antihistamine therapies. This research, like a chemist meticulously crafting a new formula, delves into the molecular structure of desloratadine, exploring its potential for therapeutic enhancement.

Desloratadine Analogues: Promise for Enhanced Antihistamine Activity

The study demonstrates that several desloratadine analogues exhibit significant antihistamine activity, potentially exceeding the effectiveness of desloratadine itself. This research, like a desert gardener cultivating a new strain of plant, reveals the potential of modifying desloratadine's structure to improve its therapeutic efficacy. This finding opens up new avenues for developing more effective and targeted antihistamine treatments.

Desloratadine Analogues: A Potential for Improved Safety and Efficacy

The study identifies compound 10, (1S,4S)-4-chlorocyclohexyl desloratadine, as a particularly promising candidate, exhibiting high antihistamine activity and a favorable safety profile. This research, like a desert explorer discovering a hidden oasis, reveals a potential new solution for alleviating allergy symptoms, offering a safer and more effective alternative to existing antihistamines.

Dr.Camel's Conclusion

This study showcases the potential of desloratadine analogues as improved antihistamine therapies, offering promising candidates with enhanced activity and potentially improved safety profiles. This research represents a significant step forward in the quest for better antihistamine treatments, providing new avenues for alleviating allergy symptoms and improving patient quality of life.

Date :
  1. Date Completed 2014-01-21
  2. Date Revised 2013-06-14
Further Info :

Pubmed ID

23719280

DOI: Digital Object Identifier

10.1016/j.bmc.2013.05.004

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Languages

English

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