Synthesis and evaluation of a 2-benzothiazolylphenylmethyl ether class of histamine H4 receptor antagonists

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• 作者：Olivier Labeeuw ; ^{o.labeeuw@bioprojet.com" class="auth_mail" title="E-mail the corresponding author} ; Nicolas Levoin ; Xavier Billot ; Denis Danvy^&dagger ; ; Thierry Calmels ; Sté ; phane Krief ; Xavier Ligneau ; Isabelle Berrebi-Bertrand ; Philippe Robert ; Jeanne-Marie Lecomte ; Jean-Charles Schwartz ; Marc Capet
• 关键词：Histamine ; Histamine H4 receptor ; Asthma ; Atopic dermatitis
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：1 November 2016
• 年：2016
• 卷：26
• 期：21
• 页码：5263-5266
• 全文大小：1779 K

文摘

Synthesis and biological evaluation of a new class of histamine H₄ receptor ligands, distinct from the previously reported chemotypes, are described. A virtual screening of our corporate compound collection identified a hit with an undesired dual H3R/H4R activity. Chemical exploration led to the discovery of a more potent and selective 2-benzothiazolylphenylmethyl ether lead compound.