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吡唑并三唑并嘧啶作为腺嘌呤受体拮抗剂：完整的构效关系。

Pyrazolo-triazolo-pyrimidines as adenosine receptor antagonists: A complete structure-activity profile.

机构信息

Dipartimento di Scienze Farmaceutiche, Università degli Studi di Ferrara, Via Fossato di Mortara 17-19, 44100, Ferrara, Italy.

出版信息

Purinergic Signal. 2007 Jun;3(3):183-93. doi: 10.1007/s11302-006-9027-x. Epub 2006 Nov 14.

DOI:10.1007/s11302-006-9027-x
PMID:18404432
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2096643/
Abstract

In the last 5 years, many efforts have been conducted searching potent and selective human A(3) adenosine antagonists. In this field several different classes of compounds, possessing very good affinity (nM range) and with a broad range of selectivity, have been proposed. Recently, our group synthesized a new series of pyrazolo-triazolo-pyrimidines bearing different substitutions at the N(5) and N(8) positions, which have been described as highly potent and selective human A(3) adenosine receptor antagonists. The present review summarizes available data and provides an overview of the structure-activity relationships found for this class of human A(3) adenosine receptor antagonists.

摘要

在过去的 5 年中，人们进行了许多努力来寻找有效且选择性高的人 A(3) 腺苷拮抗剂。在该领域中，已经提出了几种具有非常高亲和力（纳摩尔范围）和广泛选择性的不同化合物类别。最近，我们小组合成了一系列含有不同取代基的 N(5) 和 N(8) 位置的吡唑并三唑嘧啶，被描述为高活性和选择性的人 A(3) 腺苷受体拮抗剂。本综述总结了现有数据，并概述了该类人 A(3) 腺苷受体拮抗剂的结构-活性关系。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2534/2096643/324b345360bc/11302_2006_9027_Fig14_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2534/2096643/edf7e9225eea/11302_2006_9027_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2534/2096643/a9958d269d0f/11302_2006_9027_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2534/2096643/050023d06053/11302_2006_9027_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2534/2096643/d4ba88a491c1/11302_2006_9027_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2534/2096643/00dd7e4548b2/11302_2006_9027_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2534/2096643/692ff411f848/11302_2006_9027_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2534/2096643/d313d9eeda39/11302_2006_9027_Fig7_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2534/2096643/cbccf671803e/11302_2006_9027_Fig8_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2534/2096643/0963bab33dc6/11302_2006_9027_Fig9_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2534/2096643/90f6fe1d7631/11302_2006_9027_Fig10_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2534/2096643/8cf97a939816/11302_2006_9027_Fig11_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2534/2096643/cdb8e2cf7fd4/11302_2006_9027_Fig12_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2534/2096643/4a84601da272/11302_2006_9027_Fig13_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2534/2096643/324b345360bc/11302_2006_9027_Fig14_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2534/2096643/edf7e9225eea/11302_2006_9027_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2534/2096643/a9958d269d0f/11302_2006_9027_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2534/2096643/050023d06053/11302_2006_9027_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2534/2096643/d4ba88a491c1/11302_2006_9027_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2534/2096643/00dd7e4548b2/11302_2006_9027_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2534/2096643/692ff411f848/11302_2006_9027_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2534/2096643/d313d9eeda39/11302_2006_9027_Fig7_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2534/2096643/cbccf671803e/11302_2006_9027_Fig8_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2534/2096643/0963bab33dc6/11302_2006_9027_Fig9_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2534/2096643/90f6fe1d7631/11302_2006_9027_Fig10_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2534/2096643/8cf97a939816/11302_2006_9027_Fig11_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2534/2096643/cdb8e2cf7fd4/11302_2006_9027_Fig12_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2534/2096643/4a84601da272/11302_2006_9027_Fig13_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2534/2096643/324b345360bc/11302_2006_9027_Fig14_HTML.jpg

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