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

Academic Article

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• Identity
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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

Identity

International Standard Serial Number (ISSN)

• 0960-894X

Digital Object Identifier (DOI)

• 10.1016/s0960-894x(02)00356-6

PubMed ID

• 12127538

Additional Document Info

start page

• 2205

end page

• 2208

volume

• 12

issue

• 16