A new orally bioavailable dual adenosine A2B/A3 receptor antagonist with therapeutic potential

被引：26
作者：
Press, NJ
Taylor, RJ
Fullerton, JD
Tranter, P
McCarthy, C
Keller, TH
Brown, L
Cheung, R
Christie, J
Haberthuer, S
Hatto, JDI
Keenan, M
Mercer, MK
Press, NE
Sahri, H
Tuffnell, AR
Tweed, M
Fozard, JR
机构：
[1] Novartis Inst Biomed Res, Resp Dis Area, Horsham RH12 5AB, W Sussex, England
[2] Novartis Inst Biomed Res, CH-4056 Basel, Switzerland
[3] Novartis Inst Trop Dis Pte Ltd, Singapore 138670, Singapore
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 12期
关键词：
adenosine; A2B; A3; adenosine receptor antagonist; asthma; aminothiazole;
D O I：
10.1016/j.bmcl.2005.04.021
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The synthesis and SAR of 5 -heterocycle- substituted aminothiazole adenosine receptor antagonists is described. Several compounds show high affinity and selectivity for the A(2B) and A(3) receptors. One compound (5f) shows good ADME properties in the rat and as such may be an important new compound in testing the current hypotheses proposing a therapeutic role for a dual A(2B)/A(3) antagonist in allergic diseases. (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码：3081 / 3085
页数：5
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