193803-87-1Relevant academic research and scientific papers
Evaluation of endo- and exo-aryl-substitutions and central scaffold modifications on diphenyl substituted alkanes as 5-lipoxygenase activating protein inhibitors
Chu, Lin,Armstrong, Helen M.,Chang, Linda L.,Cheng, Amy F.,Colwell, Lawrence,Cui, Jisong,Evans, Jilly,Galka, Amy,Goulet, Mark T.,Hayes, Nancy,Lo, Jane,Menke, John,Ok, Hyun O.,Ondeyka, Debra L.,Patel, Minal,Quaker, Grace M.,Sings, Heather,Witkin, Stephanie L.,Zhao, Annie,Ujjainwalla, Feroze
, p. 4133 - 4138 (2012/07/03)
A search for a suitable replacement for the central norbornyl scaffold presented in the recently disclosed novel FLAP inhibitors is herein described, as well as the SAR study performed on the endo and exo-aryl groups.
RORGAMMAT INHIBITORS
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, (2012/08/28)
The present invention relates to compounds according to Formula (I) or a pharmaceutically acceptable salt or solvate thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or condition.
2,6-Substituted chroman derivatives useful as beta-3 adrenoreceptor agonists
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, (2008/06/13)
This invention relates to novel 2,6-substituted chroman derivatives which are useful in the treatment of beta-3 adrenoreceptor-mediated conditions.
Selective endothelin A receptor ligands. 1. Discovery and structure-activity of 2,4-disubstituted benzoic acid derivatives
Astles,Brown,Handscombe,Harper,Harris,Lewis,Lockey,McCarthy,McLay,Porter,Roach,Smith,Walsh
, p. 409 - 423 (2007/10/03)
This paper describes the discovery of a new non-peptide endothelin A (ET(A)) selective ligand, 2,4-dibenzyloxybenzoic acid 3, which inhibits the binding of [125I]ET-1 to ET(A) receptors with an IC50 of 9 μM (ET-1 = endothelin-1). Optimisation of 3 resulted in compound 52 which had an IC50 of 1 μM. One of the analogues of 3, compound 15, was examined in a functional assay and shown to antagonise ET-1-induced contraction of rat aorta. The identification of 3 was made through the application of ChemDBS-3D searching of our corporate database. The 3D query, using an aromatic ring to a carboxylic acid group separated by 10.2 ± 1.1 A, was derived from an examination of common pharmacophoric distances found in the low energy conformations of two known ET(A) antagonists, the cyclic pentapeptide BQ 123 1 and myriceron caffeoyl ester 2.
