In this paper we describe an extension SAR study of pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine nucleus as A3AR antagonist. Our initial aim was to replace the phenylcarbamoyl moiety at the 5 position of PTP nucleus with a thiourea functionality to evaluate the contribution of new structural modification against the A3AR. The synthesized 12-25 were not characterized by the predicted side chain but by a 1,3-disubstituted guanidine and are shown to be interesting A3AR antagonists.

One-pot reaction to obtain N,N'-disubstituted guanidines of pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine scaffold as human A3 adenosine receptor antagonists

BARALDI, Pier Giovanni
Primo
;
BARALDI, Stefania
Secondo
;
SAPONARO, Giulia;AGHAZADEH TABRIZI, Mojgan;ROMAGNOLI, Romeo;RUGGIERO, Emanuela;VINCENZI, Fabrizio;BOREA, Pier Andrea
Penultimo
;
VARANI, Katia
Ultimo
2015

Abstract

In this paper we describe an extension SAR study of pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine nucleus as A3AR antagonist. Our initial aim was to replace the phenylcarbamoyl moiety at the 5 position of PTP nucleus with a thiourea functionality to evaluate the contribution of new structural modification against the A3AR. The synthesized 12-25 were not characterized by the predicted side chain but by a 1,3-disubstituted guanidine and are shown to be interesting A3AR antagonists.
2015
Baraldi, Pier Giovanni; Baraldi, Stefania; Saponaro, Giulia; AGHAZADEH TABRIZI, Mojgan; Romagnoli, Romeo; Ruggiero, Emanuela; Vincenzi, Fabrizio; Borea, Pier Andrea; Varani, Katia
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J. Med. Chem. 2015, 58, 5355−5360.pdf

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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11392/2330161
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