Replacement of amide with bioisosteres led to a new series of potent adenosine A2A receptor antagonists

被引：15

作者：

Yang, Zhaohui

Li, Xuan

Ma, Haikuo

Zheng, Jiyue

Zhen, Xuechu

Zhang, Xiaohu ^{[1
]}

机构：

[1] Soochow Univ, Jiangsu Key Lab Translat Res & Expt Therapy Neuro, Suzhou 215021, Jiangsu, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2014年 / 24卷 / 01期

基金：

中国国家自然科学基金; 中国博士后科学基金;

关键词：

Bioisostere; Adenosine receptor; Antagonist; GPCR; Parkinson's disease; IN-VIVO EFFICACY; PARKINSONS-DISEASE; DRUG DESIGN; 2-AMINO-N-PYRIMIDIN-4-YLACETAMIDES; CLASSIFICATION; NOMENCLATURE; OPTIMIZATION; INHIBITORS; DISCOVERY;

D O I：

10.1016/j.bmcl.2013.11.051

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We have previously reported a series of 2,4,6-trisubstituted pyrimidines as potent A(2A) receptor antagonists. The leading compounds often feature a potentially labile acetamide functional group which tends to hydrolyze under acidic conditions. Here we report the replacement of the acetamide functional group with bioisosteres. This effort led us to a new series of adenosine A(2A) receptor antagonists with improved potency and chemical stability. (C) 2013 Elsevier Ltd. All rights reserved.

引用

收藏

页码：152 / 155

页数：4

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