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Modeling directed design and biological evaluation of quinazolinones as non-peptidic growth hormone secretagogues

Academic Article
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Overview

authors

  • Ye, Z. X.
  • Gao, Y. D.
  • Bakshi, R. K.
  • Chen, M. H.
  • Rohrer, S. P.
  • Feighner, S. D.
  • Pong, S. S.
  • Howard, A. D.
  • Blake, A.
  • Birzin, E. T.
  • Locco, L.
  • Parmar, R. M.
  • Chan, W. W. S.
  • Schaeffer, J. M.
  • Smith, Roy
  • Patchett, A. A.
  • Nargund, R. P.

publication date

  • January 2000

journal

  • Bioorganic & Medicinal Chemistry Letters  Journal

abstract

  • Quinazolinone derivatives were synthesized and evaluated as non-peptidic growth hormone secretagogues. Modeling guided design of quinazolinone compound 21 led to a potency enhancement of greater than 200-fold compared to human growth hormone secretagogue affinity of a screening lead 4.

subject areas

  • Animals
  • Binding Sites
  • Drug Design
  • Human Growth Hormone
  • Humans
  • Inhibitory Concentration 50
  • Kinetics
  • Models, Molecular
  • Quinazolines
  • Rats
  • Receptors, Cell Surface
  • Receptors, G-Protein-Coupled
  • Receptors, Ghrelin
  • Secretory Rate
  • Structure-Activity Relationship
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Identity

International Standard Serial Number (ISSN)

  • 0960-894X

Digital Object Identifier (DOI)

  • 10.1016/s0960-894x(99)00584-3

PubMed ID

  • 10636230
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Additional Document Info

start page

  • 5

end page

  • 8

volume

  • 10

issue

  • 1

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