Design and Synthesis of 2-Alkylpyrimidine-4,6-diol and 6-Alkylpyridine-2,4-diol as Potent GPR84 Agonists

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• 作者：Yang Liu ; Qing Zhang ; Lin-Hai Chen ; Hui Yang ; Wei Lu ; Xin Xie ; Fa-Jun Nan
• 刊名：ACS Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：June 9, 2016
• 年：2016
• 卷：7
• 期：6
• 页码：579-583
• 全文大小：325K
• 年卷期：0
• ISSN：1948-5875

文摘

A series of alkylpyrimidine-4,6-diol derivatives were designed and synthesized as novel GRP84 agonists based on a high-throughput screening (HTS) hit 1. 6-Nonylpyridine-2,4-diol was identified as the most potent agonist of GPR84 reported so far, with an EC₅₀ of 0.189 nM. These novel GPR84 agonists will provide valuable tools for the study of the physiological functions of GPR84.