108357-63-7Relevant academic research and scientific papers
Self-floating ability and initiating gradient photopolymerization of acrylamide aqueous solution of a water-soluble polysiloxane benzophenone photoinitiator
Wang, Jiansheng,Cheng, Jiye,Liu, Jiancheng,Gao, Yanjing,Sun, Fang
, p. 2457 - 2465 (2013)
Three water-soluble polysiloxane benzophenone photoinitiators (W-Si-HBP2-A/B/C) with various silicon content used for preparing a gradient polymer were synthesized based on the traditional photoinitiator 4-hydroxybenzophenone (HBP) and aminopol
Discovery of potential, dual-active histamine h3 receptor ligands with combined antioxidant properties
Kie?-Kononowicz, Katarzyna,Kotańska, Magdalena,Kuder, Kamil J.,Mika, Kamil,Reiner-Link, David,Stark, Holger,Szczepańska, Katarzyna
, (2021)
In an attempt to find new dual acting histamine H3 receptor (H3 R) ligands, we designed a series of compounds, structurally based on previously described in our group, a highly active and selective human histamine H3 receptor (hH3 R) ligand KSK63. As a result, 15 obtained compounds show moderate hH3 R affinity, the best being the compound 17 (hH3 R Ki = 518 nM). Docking to the histamine H3 R homology model revealed two possible binding modes, with key interactions retained in both cases. In an attempt to find possible dual acting ligands, selected compounds were tested for antioxidant properties. Compound 16 (hH3 R Ki = 592 nM) showed the strongest antioxidant properties at the concentration of 10?4 mol/L. It significantly reduced the amount of free radicals presenting 50–60% of ascorbic acid activity in the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay, as well as showed antioxidative properties in the ferric reducing antioxidant power (FRAP) assay. Despite the yet unknown antioxidation mechanism and moderate hH3 R affinity, 16 (QD13) constitutes a starting point for the search of potential dual acting H3 R ligands-promising tools for the treatment of neurological disorders associated with increased neuronal oxidative stress.
Structural modifications and in vitro pharmacological evaluation of 4-pyridyl-piperazine derivatives as an active and selective histamine H3 receptor ligands
Szczepańska, Katarzyna,Karcz, Tadeusz,Siwek,Kuder, Kamil J.,Latacz, Gniewomir,Bednarski,Szafarz, Ma?gorzata,Hagenow, Stefanie,Lubelska, Annamaria,Olejarz-Maciej, Agnieszka,Sobolewski, Micha?,Mika,Kotańska, Magdalena,Stark, Holger,Kie?-Kononowicz, Katarzyna
supporting information, (2019/07/31)
A novel series of 4-pyridylpiperazine derivatives with varying alkyl linker length and eastern part substituents proved to be potent histamine H3 receptor (hH3R) ligands in the nanomolar concentration range. While paying attention to
Efficacy of novel phenoxyalkyl pyridinium oximes as brain-penetrating reactivators of cholinesterase inhibited by surrogates of sarin and VX
Chambers, Janice E.,Chambers, Howard W.,Funck, Kristen E.,Meek, Edward C.,Pringle, Ronald B.,Ross, Matthew K.
, p. 154 - 159 (2016/12/06)
Pyridinium oximes are strong nucleophiles and many are effective reactivators of organophosphate-inhibited cholinesterase (ChE). However, the current oxime reactivators are ineffective at crossing the blood-brain barrier and reactivating brain ChE in the intact organism. Our laboratories have developed a series of substituted phenoxyalkyl pyridinium oximes (US patent 9,227,937 B2) with the goal of identifying reactivators effective in crossing the blood-brain barrier. The first 35 of the series were found to have similar in?vitro efficacy as reactivators of ChE inhibited by a sarin surrogate (phthalimidyl isopropyl methylphosphonate, PIMP) or a VX surrogate (nitrophenyl ethyl methylphosphonate, NEMP) in bovine brain preparations as previously observed in rat brain preparations. A number of these novel oximes have shown the ability to decrease the level of ChE inhibition in the brains of rats treated with a high sublethal dosage of either a sarin surrogate (nitrophenyl isopropyl methylphosphonate, NIMP) or the VX surrogate NEMP. Levels of reactivation at 2?h after oxime administration were up to 35% while the currently approved therapeutic, 2-PAM, yielded no reduction in brain ChE inhibition. In addition, there was evidence of attenuation of seizure-like behavior with several of the more effective novel oximes, but not 2-PAM. Therefore these novel oximes have demonstrated an ability to reactivate inhibited ChE in brain preparations from two species and in?vivo data support their ability to enter the brain and provide a therapeutic action. These novel oximes have the potential to be developed into improved antidotes for nerve agent therapy.
Synthesis, structures and properties of self-assembling quaternary ammonium dansyl fluorescent tags for porous and non-porous surfaces
Porosa, Lukasz M.,Mistry, Kamlesh B.,Mocella, Amanda,Deng, Hellen,Hamzehi, Shayan,Caschera, Alex,Lough, Alan J.,Wolfaardt, Gideon,Foucher, Daniel A.
, p. 1509 - 1520 (2014/03/21)
A series of H2O and/or EtOH soluble, self-assembling quaternary ammonium salts containing a dansyl (DNS) fluorescent moiety suitable for attachment to both porous ([DNS-NH-(CH2)3-NMe 2-R+][X-/su
UV CURED BENZOPHENONE TERMINATED QUATERNARY AMMONIUM ANTIMICROBIALS FOR SURFACES
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Page/Page column 20; 21, (2014/07/07)
The invention relates to benzophenone-terminated quaternary ammonium compounds, processes for preparing benzophenone-terminated quaternary ammonium compounds, environmentally friendly antimicrobial formulations of said quaternary ammonium compounds and th
Toward analogues of MraY natural inhibitors: Synthesis of 5′-triazole-substituted-aminoribosyl uridines through a Cu-catalyzed azide-alkyne cycloaddition
Fer, Mickael J.,Olatunji, Samir,Bouhss, Ahmed,Calvet-Vitale, Sandrine,Gravier-Pelletier, Christine
, p. 10088 - 10105 (2013/11/06)
A straightforward strategy for the synthesis of triazole-containing MraY inhibitors has been developed. It involves the sequential introduction of a terminal alkyne at the 5′ position of an uridine derivative and O-glycosylation with a protected aminoribose leading to an elaborated alkyne scaffold. An efficient Cu(I)-catalyzed azide-alkyne cycloaddition (CuAAC) allowed the introduction of chemical diversity toward a small library of inhibitors.
2-Alkoxydihydrocinnamates as PPAR agonists. Activity modulation by the incorporation of phenoxy substituents
Martín, José A.,Brooks, Dawn A.,Prieto, Lourdes,González, Rosario,Torrado, Alicia,Rojo, Isabel,López De Uralde, Beatriz,Lamas, Carlos,Ferritto, Rafael,Dolores Martín-Ortega, María,Agejas, Javier,Parra, Francisco,Rizzo, John R.,Rhodes, Gary A.,Robey, Roger L.,Alt, Charles A.,Wendel, Samuel R.,Zhang, Tony Y.,Reifel-Miller, Anne,Montrose-Rafizadeh, Chahrzad,Brozinick, Joseph T.,Hawkins, Eric,Misener, Elizabeth A.,Briere, Daniel A.,Ardecky, Robert,Fraser, James D.,Warshawsky, Alan M.
, p. 51 - 55 (2007/10/03)
Herein we describe a series of potent and selective PPARγ agonists with moderate PPARα affinity and little to no affinity for other nuclear receptors. In vivo studies in a NIDDM animal model (ZDF rat) showed that these compounds are efficacious at low doses in glucose normalization and plasma triglyceride reduction. Compound 1b (LY519818) was selected from our SAR studies to be advanced to clinical evaluation for the treatment of type II diabetes. Herein we describe a series of potent and selective PPARγ agonists with moderate PPARα affinity and little to no affinity for other nuclear receptors. In vivo studies in a NIDDM animal model (ZDF rat) showed that these compounds are efficacious at low doses in glucose normalization and plasma triglyceride reduction. Compound 1b (LY519818) was selected from our SAR studies to be advanced to clinical evaluation for the treatment of type II diabetes.
Pyrimidinedione derivatives and antiarrhythmic agents containing same
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, (2008/06/13)
Pyrimidinedione derivatives of the formula: STR1 wherein R1 and R2 is so linked with each other as to make an alkylene chain and thus form a heterocyclic structure, A, R3, R4, X1, X2 and X3 are substituents, respectively, and n is 2 or 3 have a basic backbone in which a phenyl group part and a pyrimidinedione part are linked by a structure comprising an alkyl chain and a heterocyclic ring having two nitrogen atoms. These compounds are useful for a medical treatment of cardiac arrhythmias.
Magnetic Field Effects on the Dynamics of Biradicals Generated from Benzophenone and Diphenylamine Bifunctional Chain Molecules
Tanimoto, Yoshifumi,Okada, Natsuo,Takamatsu, Shinji,Itoh, Michiya
, p. 1342 - 1348 (2007/10/02)
The magnetic field effects (MFE) on the lifetimes of triplet biradicals generated from the intramolecular photoreaction of bifunctional chain molecules, α-(4-benzoylphenoxy)-ω-alkanes (BP-O-n-O-DPA, n=2-16) were studied by laser fl
