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The design, binding affinity prediction and synthesis of macrocyclic angiotensin II AT 1 and AT 2 receptor antagonists

de Laszlo, Stephen E ; Glinka, Tomasz W ; Greenlee, William J ; Ball, Richard ; Nachbar, Robert B ; Prendergast, Kristine

Bioorganic & Medicinal Chemistry Letters, 1996, Vol.6(8), pp.923-928 [Peer Reviewed Journal]

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  • Title:
    The design, binding affinity prediction and synthesis of macrocyclic angiotensin II AT 1 and AT 2 receptor antagonists
  • Author: de Laszlo, Stephen E ; Glinka, Tomasz W ; Greenlee, William J ; Ball, Richard ; Nachbar, Robert B ; Prendergast, Kristine
  • Description: Analysis of the SAR of AT 1 selective and AT 1 AT 2 balanced affinity angiotensin II antagonists led to the design of macrocyclic quinazolinone ligands. CoMFA analysis was used to predict the binding affinities of these novel ligands. The synthesis, X-ray crystal structure, binding affinity and the relevance of these studies to the determination of the biologically relevant binding conformation is discussed. Analysis of the SAR of AT 1 selective and AT 1 AT 2 balanced affinity angiotensin II antagonists led to the design of macrocyclic quinazolinone ligands. CoMFA analysis was used to predict the binding affinities of these novel ligands. The synthesis, X-ray crystal structure, binding affinity and the relevance of these studies to the determination of the biologically relevant binding conformation is discussed.
  • Is Part Of: Bioorganic & Medicinal Chemistry Letters, 1996, Vol.6(8), pp.923-928
  • Identifier: ISSN: 0960-894X ; E-ISSN: 1464-3405 ; DOI: 10.1016/0960-894X(96)00116-3
  • Subjects: Medicine ; Chemistry ; Anatomy & Physiology
  • Language: English

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