8-Aryl-and 8-cycloalkyl-1,3-dipropylxanthines: further potent and selective antagonists for A1-adenosine receptors.

@article{Shamim19888Aryland8F,
  title={8-Aryl-and 8-cycloalkyl-1,3-dipropylxanthines: further potent and selective antagonists for A1-adenosine receptors.},
  author={M. Shamim and D. Ukena and W. Padgett and O. Hong and J. Daly},
  journal={Journal of medicinal chemistry},
  year={1988},
  volume={31 3},
  pages={
          613-7
        }
}
  • M. Shamim, D. Ukena, +2 authors J. Daly
  • Published 1988
  • Chemistry, Medicine
  • Journal of medicinal chemistry
  • A series of 1,3-dipropylxanthines were prepared with a variety of substituents at the 8-position. These included 8-aryl and 8-cycloalkyl groups. Polar carboxylate and carboxamide moieties were introduced as aryl substituents to increase water solubility. 1,3-Dipropyl-8-[2-hydroxy-4-[(carboxymethyl)oxy]phenyl]xanthine provided a functionalized congener with high potency (Ki = 37 nM) and selectivity (54-fold) for A1-adenosine receptors. This congener was used for preparation of a series of other… CONTINUE READING
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