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

Yang Liu Qing Zhang Lin-Hai Chen Hui Yang Wei Lu Xin Xie Fa-Jun Nan

ACS Med Chem Lett

State Key Laboratory of Drug Research, The National Center for Drug Screening, Shanghai Institute of Materia Medica, Chinese Academy of Sciences , 189 Guoshoujing Road, Shanghai 201203, China.

Published: June 2016

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.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4904254PMC
http://dx.doi.org/10.1021/acsmedchemlett.6b00025DOI Listing

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