Literature DB >> 10450966

Discovery of FR166124, a novel water-soluble pyrazolo-[1,5-a]pyridine adenosine A1 receptor antagonist.

S Kuroda1, A Akahane, H Itani, S Nishimura, K Durkin, T Kinoshita, Y Tenda, K Sakane.   

Abstract

Novel 3-(2-cycloalkyl and cycloalkenyl-3-oxo-2,3-dihydropyridazin-6-yl)-2-phenylpyrazo lo [1,5-a]-pyridines were synthesized and evaluated for their adenosine A1 receptor binding activities. In this series, FR166124 (3) was found to be the most potent and selective adenosine A1 receptor antagonist, and the double bond of the cyclohexenyl acetic acid group was essential for selectivity of A1 receptor binding. Furthermore, the solubility in water of the sodium salt of FR 166124 was high.

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Year:  1999        PMID: 10450966     DOI: 10.1016/s0960-894x(99)00304-2

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

Review 1.  Progress in the pursuit of therapeutic adenosine receptor antagonists.

Authors:  Stefano Moro; Zhan-Guo Gao; Kenneth A Jacobson; Giampiero Spalluto
Journal:  Med Res Rev       Date:  2006-03       Impact factor: 12.388

Review 2.  Pyrazolo derivatives as potent adenosine receptor antagonists: an overview on the structure-activity relationships.

Authors:  Siew Lee Cheong; Gopalakrishnan Venkatesan; Priyankar Paira; Ramasamy Jothibasu; Alexander Laurence Mandel; Stephanie Federico; Giampiero Spalluto; Giorgia Pastorin
Journal:  Int J Med Chem       Date:  2011-03-07
  2 in total

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