9
views
0
recommends
+1 Recommend
0 collections
    0
    shares
      • Record: found
      • Abstract: not found
      • Article: not found

      1H-Imidazo[4,5-c]quinolin-4-amines: novel non-xanthine adenosine antagonists

      Read this article at

      ScienceOpenPublisherPubMed
      Bookmark
          There is no author summary for this article yet. Authors can add summaries to their articles on ScienceOpen to make them more accessible to a non-specialist audience.

          Abstract

          On the basis of a model we recently developed for the antagonist binding site of the adenosine A1 receptor (J. Med. Chem. 1990, 33, 1708-1713), it was predicted that 1H-imidazo[4,5-c]quinolin-4-amines would be antagonists of the A1 receptor. Furthermore, it was expected that certain hydrophobic substitutions at the 2- and 4-positions would enhance affinity. Here, we report on the synthesis and the adenosine A1 and A2 receptor affinity of substituted 1H-imidazo[4,5-c]quinolin-4-amines. Some of these compounds have nanomolar affinity for the A1 receptor. The structure-activity relationships (SAR) of these compounds are discussed in relation to SAR for other adenosine receptor ligands. The 1H-imidazo[4,5-c]quinolin-4-amines constitute a novel class of non-xanthine adenosine antagonists.

          Related collections

          Author and article information

          Journal
          Journal of Medicinal Chemistry
          J. Med. Chem.
          American Chemical Society (ACS)
          0022-2623
          1520-4804
          March 1991
          March 1991
          : 34
          : 3
          : 1202-1206
          Article
          10.1021/jm00107a046
          2002461
          d233c0dd-b2e4-492a-b355-713c607ba39d
          © 1991
          History

          Comments

          Comment on this article