- Synthesis of novel isoluminol probes and their use in rapid bacterial assays
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Rapid assays for bacteria have been developed utilizing novel LysLysLys-isoluminol (14) and GluGlu-isoluminol (16) probes that have been derived from peptides which potentially mimic bacteriophage attachment protein binding regions. Compared to two conventional methods that are widely used, namely nucleic acid probes and polymerase chain reaction (PCR) assays, these types of probes may eventually have certain advantages, such as high sensitivity, and short preparation and assay time.
- Neelakantan, Sundar,Surjawan, Iwan,Karacelik, Huseyin,Hicks, Clair L.,Crooks, Peter A.
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Read Online
- Pyridyl Radical Cation for C?H Amination of Arenes
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Electron-transfer photocatalysis provides access to the elusive and unprecedented N-pyridyl radical cation from selected N-substituted pyridinium reagents. The resulting C(sp2)?H functionalization of (hetero)arenes furnishes versatile intermediates for the development of valuable aminated aryl scaffolds. Mechanistic studies that include the first spectroscopic evidence of a spin-trapped N-pyridyl radical adduct implicate SET-triggered, pseudo-mesolytic cleavage of the N?X pyridinium reagents mediated by visible light.
- R?ssler, Simon L.,Jelier, Benson J.,Tripet, Pascal F.,Shemet, Andrej,Jeschke, Gunnar,Togni, Antonio,Carreira, Erick M.
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supporting information
p. 526 - 531
(2019/01/04)
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- Development of a non-hydroxamate dual matrix metalloproteinase (MMP)-7/-13 inhibitor
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Matrix metalloproteinase 7 (MMP-7) is a member of the MMP superfamily and is able to degrade extracellular matrix proteins such as casein, gelatin, fibronectin and proteoglycan. MMP-7 is a validated target for the development of small molecule drugs against cancer. MMP-13 is within the enzyme class the most efficient contributor to type II collagen degeneration and is a validated target in arthritis and cancer. We have developed the dual MMP-7/-13 inhibitor ZHAWOC6941 with IC50-values of 2.2 μM (MMP-7) and 1.2 μM (MMP-13) that is selective over a broad range of MMP isoforms. It spares MMP-1, -2, -3, -8, -9, -12 and -14, making it a valuable modulator for targeted polypharmacology approaches.
- Fischer, Thomas,Riedl, Rainer
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- Specific fluorescence labeling of target proteins by using a ligand-4-azidophthalimide conjugate
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We herein propose a simple affinity-labeling method using a ligand-4-azidophthalimide (AzPI) conjugate. As a proof of concept, we show that two different ligand-AzPI conjugates enabled highly specific fluorescence labeling of their individual target proteins even in crude cell lysates. This method was also applied to label endogenous target proteins inside living cells.
- Chiba, Kosuke,Asanuma, Miwako,Ishikawa, Minoru,Hashimoto, Yuichi,Dodo, Kosuke,Sodeoka, Mikiko,Yamaguchi, Takao
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supporting information
p. 8751 - 8754
(2017/08/10)
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- Novel integrated carbon particle based three dimensional anodes for the electrochemical degradation of reactive dyes
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Three-dimensional carbon bed electrochemical reactors have been recently applied for the degradation of several organic pollutants. However, the carbon particles in such reactors slowly undergo attrition. We fabricated a novel flow-through three-dimensional anode using granular activated carbon (GAC) particles and polyvinylidene fluoride (PVDF) binder that potentially avoids such attrition. Optimization of the composition of GAC and PVDF with respect to mechanical integrity and electrical conductivity is reported. The anodes were tested in the electro oxidation of the reactive dyes: Reactive Orange-16 (RO-16), Reactive Red-2 (RR-2), and Reactive Blue-4 (RB-4). A tentative mechanism of dye degradation was proposed based on the observed role of the supporting electrolyte and the cyclic voltammetric, UV-vis, FT-IR and GC-MS data. The decolorization efficiencies were 75 ± 3, 81 ± 5 and 88 ± 4% for RB-4, RO-16 and RR-2, respectively. The integrated 3-D anodes are advantageous because of the absence of carbon attrition, which is otherwise found when a bed of GAC is used in the electrochemical reactors.
- Misra, Rohit,Neti, Nageswara Nao,Dionysiou, Dionysios D.,Tandekar, Mahendra,Kanade, Gajanan S.
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p. 10799 - 10808
(2015/02/05)
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- A new series of N2-substituted-5-(p-toluenesulfonylamino)phthalimide analogues as α-glucosidase inhibitors
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Several members of a new family of non-sugar-type α-glycosidase inhibitors, bearing a 5-(p-toluenesulfonylamino)phthalimide moiety and various substituent at the N2 position, were synthesized and their activities were investigated. The newly synthesized compounds displayed different inhibition profile towards yeast α-glycosidase and rat intestinal α-glycosidase. Almost all the compounds had strong inhibitory activities against yeast α-glycosidase. Regarding rat intestinal α-glycosidase, only analogs with N2-aromatic substituents displayed varying degrees of inhibitory activities on rat intestinal maltase and lactase and nearly all compounds showed no inhibition against rat intestinal α-amylase. Structure-activity relationship studies indicated that 5-(p- toluenesulfonylamino)phthalimide moiety is a favorable scaffold to exert the α-glucosidase inhibitory activity and substituents at the N2 position have considerable influence on the efficacy of the inhibition activities.
- Bian, Xiaoli,Wang, Qian,Ke, Changhu,Zhao, Guilan,Li, Yiping
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p. 2022 - 2026
(2013/04/24)
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- Bioactive peptide-based probes
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A method for preparing a site-specific peptide probe, wherein the peptide is specific to a receptor, includes modifying a marker to include a tether molecule and covalently binding the tether molecule to the peptide. The present invention also provides a labeled probe, comprising a peptide specific for a receptor and a marker. The marker is modified to include a tether molecule capable of covalently binding to the peptide. The peptide is typically derived from a bacteriophage or is a synthetic analog or derivative of the peptide. The receptor will typically be found on a surface of a bacterial cell. The method and probe of the invention are suitable for a rapid assay for a bacteria in a complex mixture.
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- Novel anilinophthalimide derivatives as potential probes for β-amyloid plaque in the brain
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A group of novel 4,5-dianilinophthalimide derivatives has been synthesized in this study for potential use as β-amyloid (Aβ) plaque probes. Staining of hippocampus tissue sections from Alzheimer's disease (AD) brain with the representative compound 9 indicated selective labeling of it to Aβ plaques. The binding affinity of radioiodinated [125I]9 for AD brain homogenates was 0.21 nM (Kd), and of other derivatives ranged from 0.9 to 19.7 nM, except for N-methyl-4,5-dianilinophthalimide (Ki > 1000 nM). [125I]9 possessed the optimal lipophilicity with Log P value of 2.16, and its in vivo biodistribution in normal mice exhibited excellent initial brain uptake (5.16% ID/g at 2 min after injection) and a fast washout rate (0.56% ID/g at 60 min). The encouraging results suggest that this novel derivative of [123I]9 may have potential as an in vivo SPECT probe for detecting amyloid plaques in the brain.
- Duan, Xin-Hong,Qiao, Jin-Ping,Yang, Yang,Cui, Meng-Chao,Zhou, Jiang-Ning,Liu, Bo-Li
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experimental part
p. 1337 - 1343
(2010/04/26)
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- 3-AZABICYCLO [3.1.0] HEXANE DERIVATIVES AS VANILLOID RECEPTOR LIGANDS
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The present invention relates to 3-azabicyclo[3.1.0]hexane derivatives, which are useful as vanilloid receptor (VR) ligands, methods of treating diseases, conditions and/or disorders modulated by vanilloid receptors with them, and processes for preparing them.
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Page/Page column 49
(2009/08/16)
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- Microenvironmental Effects of Water-Soluble Polymers on the Chemiluminescence of Luminol and Its Analogs
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The effects of water-soluble polymers(WSPs), such as bovine serum albumin(BSA) and polyethyleneimine(PEI), on chemiluminescence(CL) in an aqueous solution have been studied.The CL emission, particularly in the initial stage of the CL reaction, was strongly enhanced by increasing the concentrations of these WSPs.This was attributed to the acceleration of the chemical reactions prior to the formation of the light-emitting species.BSA was also peculiar in that it could enhance CL under neutral pH conditions.It was suggested that these WSPs offered hydrophobic and basic microenvironments well suited to the CL reaction.
- Karatani, Hajime
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p. 2023 - 2030
(2007/10/02)
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- Electron Rich Heterocycles as Donor Groups in Fluorescent Dyes
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The synthesis of N-methylphthalimides substituted with the donor groups pyrazole, triazole, benzotriazole, and naphthotriazole in position 4 is described (17, 18, 14, 12).The substituent constants of these groups are obtained by alkaline hydrolysis of the corresponding phthalimide dyes.Their solvatochromism in absorption and fluorescence gives information about charge distribution in ground- and excited state.
- Fritzsche, Katharina,Langhals, Heinz
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p. 2275 - 2286
(2007/10/02)
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