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A rational utilization of high-throughput screening affords selective, orally bioavailable 1-benzyl-3-carboxyazetidine sphingosine-1-phosphate-1 receptor agonists

Academic Article
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Overview

authors

  • Hale, J. J.
  • Lynch, C. L.
  • Neway, W.
  • Mills, S. G.
  • Hajdu, R.
  • Keohane, C. A.
  • Rosenbach, M. J.
  • Milligan, J. A.
  • Shei, G. J.
  • Parent, S. A.
  • Chrebet, G.
  • Bergstrom, J.
  • Card, D.
  • Ferrer, M.
  • Hodder, Peter
  • Strulovici, B.
  • Rosen, Hugh
  • Mandala, S.

publication date

  • December 2004

journal

  • Journal of Medicinal Chemistry  Journal

abstract

  • Moderately potent, selective S1P(1) receptor agonists identified from high-throughput screening have been adapted into lipophilic tails for a class of orally bioavailable amino acid-based S1P(1) agonists represented by 7. Many of the new compounds are potent S1P(1) agonists that select against the S1P(2), S1P(3), and S1P(4) (although not S1P(5)) receptor subtypes. Analogues 18 and 24 are highly orally bioavailable and possess excellent pharmacokinetic profiles in the rat, dog, and rhesus monkey.

subject areas

  • Administration, Oral
  • Animals
  • Azetidines
  • Biological Availability
  • CHO Cells
  • Cricetinae
  • Dogs
  • Drug Design
  • Guanosine 5'-O-(3-Thiotriphosphate)
  • Humans
  • Immunosuppressive Agents
  • Lymphocytes
  • Macaca mulatta
  • Mice
  • Rats
  • Rats, Inbred Lew
  • Receptors, Lysosphingolipid
  • Structure-Activity Relationship
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Identity

International Standard Serial Number (ISSN)

  • 0022-2623

Digital Object Identifier (DOI)

  • 10.1021/jm0492507

PubMed ID

  • 15615513
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Additional Document Info

start page

  • 6662

end page

  • 6665

volume

  • 47

issue

  • 27

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