European Journal of Medicinal Chemistry 2008-08-01

N6-1,3-diphenylurea derivatives of 2-phenyl-9-benzyladenines and 8-azaadenines: synthesis and biological evaluation as allosteric modulators of A2A adenosine receptors.

Irene Giorgi, Giuliana Biagi, Anna Maria Bianucci, Alice Borghini, Oreste Livi, Michele Leonardi, Daniele Pietra, Vincenzo Calderone, Alma Martelli

Index: Eur. J. Med. Chem. 43 , 1639-47, (2008)

Full Text: HTML

Abstract

Some 1-[4-(9-benzyl-2-phenyl-9H-purin-6-ylamino)-phenyl]-3-phenyl-urea derivatives and some 1-[4-(9-benzyl-2-phenyl-9H-8-azapurin-6-ylamino)-phenyl]-3-phenyl-urea derivatives were synthesised and evaluated for their interaction with adenosine receptors. It was found that some of these compounds can act as positive enhancers of agonist and antagonist radioligands for the A(2A) adenosine receptors. This evidence was also strengthened by functional data. Other compounds can act as negative modulators. Furthermore these compounds show inhibitory properties for A(1) and A(3) adenosine receptors.