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

ACS Med Chem Lett. 2016 Mar 30;7(6):579-83. doi: 10.1021/acsmedchemlett.6b00025. eCollection 2016 Jun 9.

Abstract

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.

Keywords: 2-alkylpyrimidine-4,6-diol; 6-alkylpyridine-2,4-diol; GPR84; agonists; structural modification.