Tricyclic xanthine derivatives containing a basic substituent: adenosine receptor affinity and drug-related properties.

ABSTRACT: A library of 27 novel amide derivatives of annelated xanthines was designed and synthesized. The new compounds represent 1,3-dipropyl- and 1,3-dibutyl-pyrimido[2,1-f]purinedione-9-ethylphenoxy derivatives including a CH₂CONH linker between the (CH₂)₂-amino group and the phenoxy moiety. A synthetic strategy to obtain the final products was developed involving solvent-free microwave irradiation. The new compounds were evaluated for their adenosine receptor (AR) affinities. The most potent derivatives contained a terminal tertiary amino function. Compounds with nanomolar AR affinities and at the same time high water-solubility were obtained (A₁ (K_i = 24-605 nM), A_2A (K_i = 242-1250 nM), A_2B</

SUBMITTER: Zaluski M 

PROVIDER: S-EPMC6071793 | biostudies-literature | 2018 Jun

REPOSITORIES: biostudies-literature