Design and Synthesis of 2-Alkylpyrimidine-4,6-diol and 6-Alkylpyridine-2,4-diol as Potent GPR84 Agonists
Design and Synthesis of 2-Alkylpyrimidine-4,6-diol and 6-Alkylpyridine-2,4-diol as Potent GPR84 Agonists
复制标题
作为有效 GPR84 激动剂的 2-烷基嘧啶-4,6-二醇和 6-烷基吡啶-2,4-二醇的设计和合成。
DOI：
10.1021/acsmedchemlett.6b00025
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发表时间：
2016-06-01
影响因子：
4.2
通讯作者：
Nan, Fa-Jun
中科院分区：
文献类型：
--
作者：
Liu, Yang;Zhang, Qing;Nan, Fa-Jun
基于高通量筛选（HTS） hit 1，设计并合成了一系列烷基嘧啶-4,6-二醇衍生物作为新型GRP84激动剂。6-壬基吡啶-2,4-二醇是目前报道的最有效的GPR84激动剂，EC50为0.189 nM。这些新型的GPR84激动剂将为研究GPR84的生理功能提供有价值的工具。
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.