36873-43-5Relevant academic research and scientific papers
SUBSTITUTED PHENOXYMETHYL DIHYDRO OXAZOLOPYRIMIDINONES, PREPARATION AND USE THEREOF
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Page/Page column 34, (2011/04/19)
The present invention relates to a series of substituted phenoxymethyl dihydro oxazolopyrimidinones of formula (I) defined herein. This invention also relates to methods of making these compounds including novel intermediates. The compounds of this invent
Synthesis and pharmacological evaluation of thieno[2,3-b]pyridine derivatives as novel c-Src inhibitors
Pevet, Isabelle,Brulé, Cédric,Tizot, André,Gohier, Arnaud,Cruzalegui, Francisco,Boutin, Jean A.,Goldstein, Solo
experimental part, p. 2517 - 2528 (2011/06/11)
Among the recently investigated targets for cancer therapy is the c-Src non-receptor tyrosine kinase. Indeed research around deregulated activity of this enzyme has proven its role in tumor progression, while the beneficial effects of c-Src inhibitors in several pathological models has also been demonstrated. We report here the preparation and pharmacological profile of a novel series of c-Src inhibitors that was elaborated around a 3-amino-thieno[2,3-b]pyridine discovered during an HTS campaign. c-Src enzyme inhibition and c-Src inhibition were investigated in a series of related compounds derived from the initial hit. Molecular modeling as well as X-ray studies on one active compound allowed us to hypothesize on ligand orientation and interactions within the ATP hydrophobic pocket. Design and synthesis of structural analogs then led to new ligands possessing quite efficient enzymatic and c-Src inhibition. The structure-activity elements disclosed in this study shed light on the role played by substituents on the thienopyridine ring as well as the impact of other aromatic moieties in the molecule when interacting with the enzyme.
[1,2,4]THIADIAZINE 1,1-DIOXIDE COMPOUNDS
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Page/Page column 64, (2009/12/24)
The invention is directed to [1,2,4]thiadiazine 1,1-dioxide compounds and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.
Structure-activity relationships of the peptide deformylase inhibitor BB-3497: Modification of the methylene spacer and the P1′ side chain
Davies, Stephen J.,Ayscough, Andrew P.,Beckett, R. Paul,Bragg, Ryan A.,Clements, John M.,Doel, Sheila,Grew, Christine,Launchbury, Steven B.,Perkins, Gemma M.,Pratt, Lisa M.,Smith, Helen K.,Spavold, Zoe M.,Thomas, S. Wayne,Todd, Richard S.,Whittaker, Mark
, p. 2709 - 2713 (2007/10/03)
Structural modifications to the peptide deformylase inhibitor BB-3497 are described. In this paper, we describe the initial SAR around this lead for modifications to the methylene spacer and the P1′ side chain. Enzyme inhibition and antibacterial activity data revealed that the optimum distance between the N-formyl hydroxylamine metal binding group and the P1′ side chain is one unsubstituted methylene unit. Additionally, lipophilic P1′ side chains that closely mimic the methionine residue in the substrate provided compounds with the best microbiological profile.
