15382-15-7Relevant academic research and scientific papers
Facile preparation of fused ring azolylureas
Drumm, Joseph E.,Deininger, David D.,LeTiran, Arnaud,Wang, Tiansheng,Grillot, Anne-Laure,Liao, Yusheng,Ronkin, Steven M.,Stamos, Dean P.,Tang, Qing,Tian, Shi-Kai,Oliver-Shaffer, Patricia
, p. 5535 - 5538 (2007)
Two novel reagents for the preparation of fused ring azolylureas are presented.
Discovery and Optimization of Isoquinoline Ethyl Ureas as Antibacterial Agents
Panchaud, Philippe,Bruyère, Thierry,Blumstein, Anne-Catherine,Bur, Daniel,Chambovey, Alain,Ertel, Eric A.,Gude, Markus,Hubschwerlen, Christian,Jacob, Lo?c,Kimmerlin, Thierry,Pfeifer, Thomas,Prade, Lars,Seiler, Peter,Ritz, Daniel,Rueedi, Georg
supporting information, p. 3755 - 3775 (2017/05/19)
Our strategy to combat resistant bacteria consisted of targeting the GyrB/ParE ATP-binding sites located on bacterial DNA gyrase and topoisomerase IV and not utilized by marketed antibiotics. Screening around the minimal ethyl urea binding motif led to the identification of isoquinoline ethyl urea 13 as a promising starting point for fragment evolution. The optimization was guided by structure-based design and focused on antibacterial activity in vitro and in vivo, culminating in the discovery of unprecedented substituents able to interact with conserved residues within the ATP-binding site. A detailed characterization of the lead compound highlighted the potential for treatment of the problematic fluoroquinolone-resistant MRSA, VRE, and S. pneumoniae, and the possibility to offer patients an intravenous-to-oral switch therapy was supported by the identification of a suitable prodrug concept. Eventually, hERG K-channel block was identified as the main limitation of this chemical series, and efforts toward its minimization are reported.
BENZOARYLUREIDO COMPOUNDS, AND COMPOSITION FOR PREVENTION OR TREATMENT OF NEURODEGENERATIVE BRAIN DISEASE CONTAINING THE SAME
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Page/Page column 5; 12, (2012/01/13)
Novel benzoarylureido compounds and a use thereof for prevention and/or treatment of the neurodegenerative brain disease are provided. The neurodegenerative brain diseases may include Alzheimer's disease, dementia, Parkinson's disease, stroke, amyloidosis, Pick's disease, Lou Gehrig's disease, Huntington's disease, Creutzfeld-Jakob disease, and the like.
BENZOARYLUREIDO COMPOUNDS, AND COMPOSITION FOR PREVENTION OR TREATMENT OF NEURODEGENERATIVE BRAIN DISEASE CONTAINING THE SAME
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Page/Page column 27, (2010/08/04)
Novel benzoarylureido compounds and a use thereof for prevention and/or treatment of the neurodegenerative brain disease are provided. The neurodegenerative brain diseases may include Alzheimer's disease, dementia, Parkinson's disease, stroke, amyloidosis, Pick's disease, Lou Gehrig's disease, Huntington's disease, Creutzfeld-Jakob disease, and the like.
UREA DERIVATIVES AND THEIR USE AS ANTI-INFLAMMATORY AGENTS
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Page 11; 18, (2008/06/13)
The present invention provides compositions and their use in the treatment of inflammatory diseases caused by T-cell proliferation such as sepsis, inflammatory bowel diseases, autoimmune encephalomyelitis, or lupus. The compositions comprise disubstituted
