SYNTHESIS OF NEW PYRAZOLO[4,3-E]1,2,4-TRIAZOLO[1,5-C] PYRIMIDINE AND 1,2,3-TRIAZOLO[4,5-E]1,2,4-TRIAZOLO[1,5-C] PYRIMIDINE DISPLAYING POTENT AND SELECTIVE ACTIVITY AS A(2A) ADENOSINE RECEPTOR ANTAGONISTS

被引：78

作者：

BARALDI, PG ^{[1
]}

MANFREDINI, S ^{[1
]}

SIMONI, D ^{[1
]}

ZAPPATERRA, L ^{[1
]}

ZOCCHI, C ^{[1
]}

DIONISOTTI, S ^{[1
]}

ONGINI, E ^{[1
]}

机构：

[1] SCHERING PLOUGH SPA,RIC LAB,I-20060 COMAZZO,ITALY

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1994年 / 4卷 / 21期

关键词：

D O I：

10.1016/S0960-894X(01)80279-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidines and 1,2,3-triazolo[4,5-e]1,2,4-triazolo[1,5-c]pyrimidines were prepared and evaluated for their activity as adenosine A(2a) receptor antagonists. In the present study, 5-amino-7-(phenylethyl)-2-(2-furyl)-pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine 7d (SCH 58261) was identified as potent and selective adenosine Aza antagonist in binding assays (Ki = 2.3 nM, Ki ratio: A(1)/A(2a) = 52.6).

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页码：2539 / 2544

页数：6

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