177977-33-2Relevant academic research and scientific papers
The design, binding affinity prediction and synthesis of macrocyclic angiotensin II AT1 and AT2 receptor antagonists
De Laszlo, Stephen E.,Glinka, Tomasz W.,Greenlee, William J.,Ball, Richard,Nachbar, Robert B.,Prendergast, Kristine
, p. 923 - 928 (2007/10/03)
Analysis of the SAR of AT1 selective and AT1/AT2 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.
