Structure-affinity relationships of the affinity of 2-pyrazolyl adenosine analogues for the adenosine A2A receptor

被引：29

作者：

Palle, VP

Elzein, EO

Gothe, SA

Li, ZH

Gao, ZH

Meyer, S

Blackburn, B

Zablocki, JA

机构：

[1] CV Therapeut, Dept Bioorgan Chem, Palo Alto, CA 94304 USA

[2] CV Therapeut, Dept Pharmacol Sci, Palo Alto, CA 94304 USA

[3] Tripos Inc, San Francisco, CA USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 20期

关键词：

D O I：

10.1016/S0960-894X(02)00609-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The structure-affinity relationships of two novel 2-substituted adenosine series containing a substituted pyrazole attached at the N-1 or C-4 position for the adenosine (ADO) A(2A) receptor are described. Compounds in the 2-(N-1-pyrazolyl) adenosine series IV provided the highest affinity for the ADO A(2A) receptor as compared to the 2-(C-4-pyrazolyl) series V. The main structural differences between the two series point to the N-1 nitrogen of series IV imparting more favorable binding interactions with the receptor than those of series V. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：2935 / 2939

页数：5

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