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

doi:10.1021/acsmedchemlett.6b00025

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

^*Corresponding author for this work

School of Chemistry and Molecular Engineering

Research output: Contribution to journal › Article › peer-review

42 Scopus citations

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.

Original language	English
Pages (from-to)	579-583
Number of pages	5
Journal	ACS Medicinal Chemistry Letters
Volume	7
Issue number	6
DOIs	https://doi.org/10.1021/acsmedchemlett.6b00025
State	Published - 9 Jun 2016

Keywords

2-alkylpyrimidine-4,6-diol
6-alkylpyridine-2,4-diol
GPR84
agonists
structural modification

Access to Document

10.1021/acsmedchemlett.6b00025

Cite this

@article{1f7b1cdd5f024ea0bdee2d449fa27b0e,

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

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",

author = "Yang Liu and Qing Zhang and Chen, \{Lin Hai\} and Hui Yang and Wei Lu and Xin Xie and Nan, \{Fa Jun\}",

note = "Publisher Copyright: {\textcopyright} 2016 American Chemical Society.",

year = "2016",

month = jun,

day = "9",

doi = "10.1021/acsmedchemlett.6b00025",

language = "英语",

volume = "7",

pages = "579--583",

journal = "ACS Medicinal Chemistry Letters",

issn = "1948-5875",

publisher = "American Chemical Society",

number = "6",

}

TY - JOUR

T1 - Design and Synthesis of 2-Alkylpyrimidine-4,6-diol and 6-Alkylpyridine-2,4-diol as Potent GPR84 Agonists

AU - Liu, Yang

AU - Zhang, Qing

AU - Chen, Lin Hai

AU - Yang, Hui

AU - Lu, Wei

AU - Xie, Xin

AU - Nan, Fa Jun

PY - 2016/6/9

Y1 - 2016/6/9

N2 - 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.

AB - 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.

KW - 2-alkylpyrimidine-4,6-diol

KW - 6-alkylpyridine-2,4-diol

KW - GPR84

KW - agonists

KW - structural modification

UR - https://www.scopus.com/pages/publications/84974621139

U2 - 10.1021/acsmedchemlett.6b00025

DO - 10.1021/acsmedchemlett.6b00025

M3 - 文章

AN - SCOPUS:84974621139

SN - 1948-5875

VL - 7

SP - 579

EP - 583

JO - ACS Medicinal Chemistry Letters

JF - ACS Medicinal Chemistry Letters

IS - 6

ER -

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

Abstract

Keywords

Access to Document

Other files and links

Fingerprint

Cite this