223388-20-3Relevant academic research and scientific papers
Application of a proteolysis/mass spectrometry method for investigating the effects of inhibitors on hydroxylase structure
Stubbs, Christopher J.,Loenarz, Christoph,Mecinovi?, Jasmin,Kar, Kheng Yeoh,Hindley, Nicola,Liénard, Beno?t M.,Sobott, Frank,Schofield, Christopher J.,Flashman, Emily
, p. 2799 - 2805 (2009)
Limited proteolysis coupled to matrix-assisted laser desorption/ionization (MALDI) mass spectrometric analyses can be used to screen for compounds that alter protein structure by monitoring stabilizing/destabilizing effects with respect to the rate and na
Using NMR solvent water relaxation to investigate metalloenzyme - Ligand binding interactions
Leung, Ivanhoe K. H.,Flashman, Emily,Yeoh, Kar Kheng,Schofield, Christopher J.,Claridge, Timothy D. W.
supporting information; experimental part, p. 867 - 875 (2010/07/05)
This report demonstrates that solvent water relaxation measurements can be used for quantitative screening of ligand binding and for mechanistic investigations of enzymes containing paramagnetic metal centers by using conventional NMR instrumentation at high field. The method was exemplified using prolyl hydroxylase domain containing enzyme 2 (PHD2), a human enzyme involved in hypoxic sensing, with Mn(II) substituting for Fe(II) at the active site. KD values were determined for inhibitors that hinder access of water to the paramagnetic center. This technique is also useful for investigating the mechanism of suitable metalloenzymes, including order of ligand binding and modes of inhibition. 2009 American Chemical Society.
3-Hydroxyisoquinolines as inhibitors of HCV NS5b RNA-dependent RNA polymerase
Hendricks, Robert T.,Spencer, Stacey R.,Blake, James F.,Fell, Jay B.,Fischer, John P.,Stengel, Peter J.,Leveque, Vincent J.P.,LePogam, Sophie,Rajyaguru, Sonal,Najera, Isabel,Josey, John A.,Swallow, Steven
scheme or table, p. 410 - 414 (2011/03/18)
Isoquinoline-based non-nucleoside inhibitors of HCV NS5b RNA-dependent RNA-polymerase are described. The synthesis and structure-activity relationships are detailed, along with enzyme and cellular activity.
Heterocyclic antiviral compounds
-
Page/Page column 28, (2008/06/13)
Compounds having the formula I wherein A, m and R1 are herein defined are Hepatitis C virus polymerase inhibitors. Also disclosed are compositions and methods for treating diseases mediated by HCV and for inhibiting hepatitis replication. Also disclosed are processes for making the compounds and synthetic intermediates used in the process
Heterocyclic antiviral compounds
-
Page/Page column 18; 30, (2010/11/24)
Compounds having the formula I wherein A, m and R1 are herein defined are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for inhibiting hepatitis replication, processes for making the compounds and syn
Substituted isoquinoline-3-carboxamides, their preparation and their use as pharmaceuticals
-
, (2008/06/13)
Novel isoquinoline-3-carboxamides of the formula I: in which R1 is hydrogen or chlorine, R2 is hydrogen, alkyl, alkoxy, chlorine, trifluoromethyl, hydroxyl, or benzyloxy which is optionally substituted, or fluoroalkoxy of the formula O-[CH2]x-CfH(2f+1-g)Fg, where x=0 or 1, f=1-5, and g=1 to (2f+1), R3 is hydrogen, alkyl, alkoxy, fluorine, chlorine, cyano, trifluoromethyl, hydroxyl, or benzyloxy which is optionally substituted, or fluoroalkoxy of the above formula, R4 and R5 are hydrogen, alkyl, fluorine, chlorine, bromine, trifluoromethyl, cyano, alkoxy, or fluoroalkoxy of the above formula, including the physiologically active salts, are strong prolyl-4-hydroxylase inhibitors which do not cause steatosis.
