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Design, synthesis, and evaluation of oxazole transthyretin amyloidogenesis inhibitors

Academic Article
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Overview

related to degree

  • Chiang, Kyle Ping, Ph.D. in Macromolecular and Cellular Structure and Chemistry, Scripps Research 2001 - 2006
  • Purkey, Hans, Ph.D. in Biology, Scripps Research 1996 - 2002

authors

  • Razavi, H.
  • Powers, Evan
  • Purkey, Hans
  • Adamski-Werner, S. L.
  • Chiang, Kyle Ping
  • Dendle, M. T. A.
  • Kelly, Jeffery

publication date

  • February 2005

journal

  • Bioorganic & Medicinal Chemistry Letters  Journal

abstract

  • Ten oxazoles bearing a C(4) carboxyl group were synthesized and evaluated as transthyretin (TTR) amyloid fibril inhibitors. Substituting aryls at the C(2) position of the oxazole ring reveals that a 3,5-dichlorophenyl substituent significantly reduced amyloidogenesis. The efficacy of these inhibitors was enhanced further by installing an ethyl, a propyl, or a CF(3) group at the C(5) position. The CF(3) substitution at C(5) also improves the TTR binding selectivity over all the other proteins in human blood.

subject areas

  • Amyloid
  • Blood Proteins
  • Drug Design
  • Humans
  • Oxazoles
  • Prealbumin
  • Structure-Activity Relationship
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Research

keywords

  • amyloidogenesis inhibitors
  • aryl oxazole
  • inhibitor binding selectivity
  • transthyretin
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Identity

International Standard Serial Number (ISSN)

  • 0960-894X

Digital Object Identifier (DOI)

  • 10.1016/j.bmcl.2004.12.022

PubMed ID

  • 15686915
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Additional Document Info

start page

  • 1075

end page

  • 1078

volume

  • 15

issue

  • 4

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