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 A2a 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 A2a antagonist in binding assays (Ki = 2.3 nM, Ki ratio: A1/A2a = 52.6).

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 A2a adenosine receptor antagonists

BARALDI, Pier Giovanni;MANFREDINI, Stefano;SIMONI, Daniele;
1994

Abstract

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 A2a 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 A2a antagonist in binding assays (Ki = 2.3 nM, Ki ratio: A1/A2a = 52.6).
1994
Baraldi, Pier Giovanni; Manfredini, Stefano; Simoni, Daniele; Zappaterra, Laura; Zocchi, Cristina; Dionisotti, Silvio; Ongini, Ennio
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11392/460434
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