89951-56-4Relevant academic research and scientific papers
Chemoselective reduction of nitroarenes, N-acetylation of arylamines, and one-pot reductive acetylation of nitroarenes using carbon-supported palladium catalytic system in water
Zeynizadeh, Behzad,Mohammad Aminzadeh, Farkhondeh,Mousavi, Hossein
, p. 3289 - 3312 (2021/05/11)
Developing and/or modifying fundamental chemical reactions using chemical industry-favorite heterogeneous recoverable catalytic systems in the water solvent is very important. In this paper, we developed convenient, green, and efficient approaches for the chemoselective reduction of nitroarenes, N-acetylation of arylamines, and one-pot reductive acetylation of nitroarenes in the presence of the recoverable heterogeneous carbon-supported palladium (Pd/C) catalytic system in water. The utilize of the simple, effective, and recoverable catalyst and also using of water as an entirely green solvent along with relatively short reaction times and good-to-excellent yields of the desired products are some of the noticeable features of the presented synthetic protocols. Graphic abstract: [Figure not available: see fulltext.].
Selective Triazenation Reaction (STaR) of Secondary Amines for Tagging Monomethyl Lysine Post-Translational Modifications
Nwajiobi, Ogonna,Mahesh, Sriram,Streety, Xavier,Raj, Monika
supporting information, p. 7344 - 7352 (2021/03/01)
Lysine monomethylation (Kme) is an impactful post-translational modification (PTM) responsible for regulating biological processes and implicated in diseases, thus there is great interest in identifying these methylation marks globally. However, the progr
New hits as antagonists of GPR103 identified by HTS
Nordqvist, Anneli,Kristensson, Lisbeth,Johansson, Kjell E.,Isaksson Da Silva, Krystle,Fex, Tomas,Tyrchan, Christian,Svensson Henriksson, Anette,Nilsson, Kristina
, p. 527 - 532 (2014/06/09)
Preclinical data indicate that GPR103 receptor and its endogenous neuropeptides QRFP26 and QRFP43 are involved in appetite regulation. A high throughput screening (HTS) for small molecule GPR103 antagonists was performed with the clinical goal to target weight management by modulation of appetite. A high hit rate from the HTS and initial low confirmation with respect to functional versus affinity data challenged us to revise the established screening cascade. To secure high quality data while increasing throughput, the binding assay was optimized on quality to run at single concentration. This strategy enabled evaluation of a larger fraction of chemical clusters and singletons delivering 17 new compound classes for GPR103 antagonism. Representative compounds from three clusters are presented. One of the identified clusters was further investigated, and an initial structure-activity relationship study is reported. The most potent compound identified had a pIC50 of 7.9 with an improved ligand lipophilic efficiency.
KINASE INHIBITORS
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Paragraph 0503; 0504, (2015/01/06)
Compounds of formula (I) described herein are p38 MAPK inhibitors and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract
KINASE INHIBITORS
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Page/Page column 108, (2015/01/06)
This invention relates to compounds and compositions that are p38 MAPK inhibitors, useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. identification of a suitable "back-up" compound for N-tert-butyl isoquine
O'Neill, Paul M.,Shone, Alison E.,Stanford, Deborah,Nixon, Gemma,Asadollahy, Eghbaleh,Park, B. Kevin,Maggs, James L.,Roberts, Phil,Stocks, Paul A.,Biagini, Giancarlo,Bray, Patrick G.,Davies, Jill,Berry, Neil,Hall, Charlotte,Rimmer, Karen,Winstanley, Peter A.,Hindley, Stephen,Bambal, Ramesh B.,Davis, Charles B.,Bates, Martin,Gresham, Stephanie L.,Brigandi, Richard A.,Gomez-de-las-Heras, Federico M.,Gargallo, Domingo V.,Parapini, Silvia,Vivas, Livia,Lander, Hollie,Taramelli, Donatella,Ward, Stephen A.
supporting information; experimental part, p. 1828 - 1844 (2009/12/31)
On the basis of a mechanistic understanding of the toxicity of the 4-aminoquinoline amodiaquine (1b), three series of amodiaquine analogues have been prepared where the 4-aminophenol "metabolic alert" has been modified by replacement of the 4'-hydroxy gro
3-Mercaptopropionic acids as efficacious inhibitors of activated thrombin activatable fibrinolysis inhibitor (TAFIa)
Islam, Imadul,Bryant, Judi,May, Karen,Mohan, Raju,Yuan, Shendong,Kent, Lorraine,Morser, John,Zhao, Lei,Vergona, Ron,White, Kathy,Adler, Marc,Whitlow, Marc,Buckman, Brad O.
, p. 1349 - 1354 (2007/10/03)
A novel series of cyclic potent, selective, small molecule, thiol-based inhibitors of activated thrombin activatable fibrinolysis inhibitor (TAFIa) and the crystal structures of TAFIa inhibitors bound to porcine pancreatic carboxypeptidase B are described. Three series of cyclic arginine and lysine mimetic inhibitors vary significantly in their selectivity against other human basic carboxypeptidases, carboxypeptidase N and carboxypeptidase B. (-)2a displays TAFIa IC50 = 3 nM and 600-fold selectivity against CPN. Inhibition of TAFIa with (rac)2a resulted in dose dependent acceleration of human plasma clot lysis in vitro and was efficacious as an adjunct to tPA in an in vivo rabbit jugular vein thrombolysis model.
ORGANIC COMPOUNDS
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Page/Page column 49, (2008/06/13)
The present invention relates to quinazolinone compounds of the formula wherein R2, R3, R5, R6 R7 and R8 are as defined in the specification and in the claims, in free form or in salt form , processes for their preparation and their use as pharmaceuticals, particularly in the treatment of disorders ameliorated by administration of TRPV1 antagonists.
New macrobicyclic triphosphazides and triphosphazenes formed by self-assembly of tripodal triazides with triphosphanes
Alajarín, Mateo,López-Leonardo, Carmen,Berná, José
, p. 6190 - 6202 (2007/10/03)
The self-assembly of tris(3-azidobenzyl)amines with 1,1,1-tris[(diphenylphosphino)methyl]ethane via tripod-tripod coupling proceeds successfully to give chiral macrobicyclic triphosphazides. The heating of these macrobicyclic cages induces a remarkable stepwise triple extrusion of molecular nitrogen to afford tri-λ5-phosphazenes, which preserved the chiral, propeller-like topology of their precursors. The replacement of one benzylic arm by an ortho-phenethylic or propylenic one still allows the success of the self-assembly. However, the quaternization of the pivotal nitrogen atom of the triamine in the form of N-oxide prevented its coupling with the triphosphane.
The structural influence in the stability of polymer-bound diazonium salts
Braese, Stefan,Dahmen, Stefan,Popescu, Crisan,Schroen, Maarten,Wortmann, Franz-Josef
, p. 5285 - 5296 (2007/10/03)
Various new diazonium ions on a polymeric support that have a variety of counterions and complexation with crown ethers have been prepared, and the thermal stability of these resins over a larger temperature interval has been investigated. Nonisothermal k
