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Identification and initial structure-activity relationships of a novel non-peptide quinolone GnRH receptor antagonist

Academic Article
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Overview

authors

  • DeVita, R. J.
  • Hollings, D. D.
  • Goulet, M. T.
  • Wyvratt, M. J.
  • Fisher, M. H.
  • Lo, J. L.
  • Yang, Y. T.
  • Cheng, K.
  • Smith, Roy

publication date

  • 1999

journal

  • Bioorganic & Medicinal Chemistry Letters  Journal

abstract

  • Screening of the Merck sample collection for non-peptide compounds with binding affinity for the rat GnRH receptor led to the identification of the substituted quinolone (1) as a lead compound in the search for a non-peptide GnRH receptor antagonist. Substantial improvements in potency (approximately 300 fold) were achieved by addition of an alkyl amine at the 4-position, a 3,5-dimethylphenyl group at the 3-position and 6-nitro-7-chloro-substitution of the 1 H-quinolone core.

subject areas

  • Animals
  • Protein Binding
  • Quinolones
  • Rats
  • Receptors, LHRH
  • Structure-Activity Relationship
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Identity

International Standard Serial Number (ISSN)

  • 0960-894X

Digital Object Identifier (DOI)

  • 10.1016/s0960-894x(99)00446-1

PubMed ID

  • 10498220
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Additional Document Info

start page

  • 2615

end page

  • 2620

volume

  • 9

issue

  • 17

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