Synthesis and SAR evaluation of 1,2,4-triazoles as A2A receptor antagonists

被引：30

作者：

Alanine, A

Anselm, L

Steward, L

Thomi, S

Vifian, W

Groaning, MD

机构：

[1] F Hoffmann La Roche & Cie AG, Pharmaceut Div, Discovery Chem, Lead Generat, CH-4070 Basel, Switzerland

[2] F Hoffmann La Roche & Cie AG, Pharmaceut Div, Discovery Biol, Cent Nervous Syst Disorders, CH-4070 Basel, Switzerland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 03期

关键词：

1,2,4-triazoles; A2A receptor antagonists; SAR;

D O I：

10.1016/j.bmcl.2003.09.095

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis and in vitro structure-activity relationships (SAR) of a series of triazoles as A(2A) receptor antagonists is reported. This resulted in the identification of potent, selective and permeable 1,2,4-triazoles such as A(2A) for further optimization and evaluation in vivo. (C) 2003 Elsevier Ltd. All rights reserved.

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页码：817 / 821

页数：5

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