张小虎教授课题组在Bioorg. Med. Chem. Lett.发表科研论文

Replacement of amide with bioisosteres led to a new series of potent adenosine A2A receptor antagonists
Zhaohui Yang, Xuan Li, Haikuo Ma, Jiyue Zheng, Xuechu Zhen, Xiaohu Zhang*
Bioorg. Med. Chem. Lett., 2014, 24, 152-155 (IF=2.338)

Abstract: We have previously reported a series of 2,4,6-trisubstituted pyrimidines as potent A2A 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 A2A receptor antagonists with improved potency and chemical stability.