25829-61-2Relevant academic research and scientific papers
Construction of a family of biphenyl combinatorial libraries: Structure- activity studies utilizing libraries of mixtures
Neustadt, Bernard R.,Smith, Elizabeth M.,Lindo, Neil,Nechuta, Terry,Bronnenkant, Alan,Wu, Arthur,Armstrong, Lydia,Kumar, Chandra
, p. 2395 - 2398 (2007/10/03)
A set of biphenyl aminoacid building blocks has been synthesized. These were used to construct partially-peptidic combinatorial libraries as equimolar multi-component samples. Activity of members of this library as vitronectin receptor antagonists is described, together with SAR studies of the most active members. These studies illustrate several important features of combinatorial libraries.
Nonpeptide arginine vasopressin antagonists for both V(1A) and V2 receptors: Synthesis and pharmacological properties of 2-Phenyl-4'- [(2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl)carbonyl]benzanilide derivatives
Matsuhisa, Akira,Tanaka, Akihiro,Kikuchi, Kazumi,Shimada, Yoshiaki,Yatsu, Takeyuki,Yanagisawa, Isao
, p. 1870 - 1874 (2007/10/03)
A series of compounds structurally related to 4'-[(2,3,4,5-tetrahydro- 1H-1-benzazepin-1-yl)carbonyl]benzanilide was synthesized and demonstrated to have arginine vasopressin (AVP) antagonist activity for both V(1A) and V2 receptors. The introduction of a phenyl or a 4-substituted phenyl group into the ortho position of the benzoyl moiety resulted in an increase in both binding affinity and antagonistic activity. The 2-(4-methylphenyl) derivative (1g) exhibited high antagonistic activities for both V(1A) (8.6- fold) and V2 (38-fold) receptors and high oral activity (8.6-fold) compared with the 2-methyl lead compound (1a). Detail of the synthesis and the pharmacological properties of this series are presented.
