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).File in questo prodotto:
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