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N-aryl-prolyl-dipeptides as potent antagonists of VLA-4

Academic Article
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Overview

authors

  • Kamenecka, Theodore
  • Lanza, T.
  • de Laszlo, S. E.
  • Li, B.
  • McCauley, E. D.
  • Van Riper, G.
  • Egger, L. A.
  • Kidambi, U.
  • Mumford, R. A.
  • Tong, S.
  • MacCoss, M.
  • Schmidt, J. A.
  • Hagmann, W. K.

publication date

  • August 2002

journal

  • Bioorganic & Medicinal Chemistry Letters  Journal

abstract

  • The design, synthesis, and biological evaluation of N-arylprolyl-dipeptide derivatives as small molecule VLA-4 antagonists is described. Potency against VLA-4 and alpha(4)beta(7) and rat pharmacokinetic evaluation revealed some advantages over the related N-(arylsulfonyl)-prolyl-dipeptide analogues.

subject areas

  • Animals
  • Dipeptides
  • Half-Life
  • Integrin alpha4beta1
  • Metabolic Clearance Rate
  • Molecular Structure
  • Rats
  • Rats, Sprague-Dawley
  • Structure-Activity Relationship
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Identity

International Standard Serial Number (ISSN)

  • 0960-894X

Digital Object Identifier (DOI)

  • 10.1016/s0960-894x(02)00356-6

PubMed ID

  • 12127538
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Additional Document Info

start page

  • 2205

end page

  • 2208

volume

  • 12

issue

  • 16

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