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Discovery of diazepane amide DORAs and 2-SORAs enabled by exploration of isosteric quinazoline replacements

Academic Article
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Overview

authors

  • Roecker, Anthony
  • Mercer, S. P.
  • Bergman, J. M.
  • Gilbert, K. F.
  • Kuduk, S. D.
  • Harrell, C. M.
  • Garson, S. L.
  • Fox, S. V.
  • Gotter, A. L.
  • Tannenbaum, P. L.
  • Prueksaritanont, T.
  • Cabalu, T. D.
  • Cui, D.
  • Lemaire, W.
  • Winrow, C. J.
  • Renger, J. J.
  • Coleman, P. J.

publication date

  • November 2015

journal

  • Bioorganic & Medicinal Chemistry Letters  Journal

subject areas

  • Animals
  • Disease Models, Animal
  • Dogs
  • Dose-Response Relationship, Drug
  • Drug Discovery
  • Humans
  • Mice
  • Microsomes, Liver
  • Models, Molecular
  • Molecular Structure
  • Orexin Receptor Antagonists
  • Orexin Receptors
  • Pyrimidines
  • Quinazolines
  • Rats
  • Sleep Initiation and Maintenance Disorders
  • Structure-Activity Relationship
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Research

keywords

  • Antagonists
  • Isostere
  • Orexin
  • Quinazoline
  • Sleep
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Identity

International Standard Serial Number (ISSN)

  • 0960-894X

Digital Object Identifier (DOI)

  • 10.1016/j.bmcl.2014.12.081

PubMed ID

  • 25613676
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Additional Document Info

start page

  • 4992

end page

  • 4999

volume

  • 25

issue

  • 21

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