1, 8-Disubstituted xanthine derivatives: synthesis of potent A2B-selective adenosine receptor antagonists

…, J Sandoval-Ramírez, U Reith, U Schobert…

Index: Hayallah, Alaa M.; Sandoval-Ramirez, Jesus; Reith, Ulrike; Schobert, Ulrike; Preiss, Birgit; Schumacher, Britta; Daly, John W.; Mueller, Christa E. Journal of Medicinal Chemistry, 2002 , vol. 45, # 7 p. 1500 - 1510

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Citation Number: 117

Abstract

3-Unsubstituted xanthine derivatives bearing a cyclopentyl or a phenyl residue in the 8- position were synthesized and developed as A2B adenosine receptor antagonists. Compounds bearing polar substituents were prepared to obtain water-soluble derivatives. 1- Alkyl-8-phenylxanthine derivatives were found to exhibit high affinity for A2B adenosine receptors (ARs). 1, 8-Disubstituted xanthine derivatives were equipotent to or more potent ...