- Electrochemical driven water oxidation by molecular catalysts in situ polymerized on the surface of graphite carbon electrode
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A simple strategy to immobilize highly efficient ruthenium based molecular water-oxidation catalysts on the basal-plane pyrolytic graphite electrode (BPG) by polymerization has been demonstrated. The electrode 1@BPG has obtained a high initial turnover frequency (TOF) of 10.47 s-1 at ~700 mV overpotential, and a high turnover number (TON) up to 31600 in 1 h electrolysis.
- Wang, Lei,Fan, Ke,Daniel, Quentin,Duan, Lele,Li, Fusheng,Philippe, Bertrand,Rensmo, H?kan,Chen, Hong,Sun, Junliang,Sun, Licheng
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supporting information
p. 7883 - 7886
(2015/05/05)
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- 4-alkyloxyimino derivatives of uridine-5′-triphosphate: Distal modification of potent agonists as a strategy for molecular probes of P2Y 2, P2Y4, and P2Y6 receptors
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Extended N4-(3-arylpropyl)oxy derivatives of uridine-5′-triphosphate were synthesized and potently stimulated phospholipase C stimulation in astrocytoma cells expressing G protein-coupled human (h) P2Y receptors (P2YRs) activated by UTP (P2Y2/4R) or UDP (P2Y6R). The potent P2Y4R-selective N4-(3- phenylpropyl)oxy agonist was phenyl ring-substituted or replaced with terminal heterocyclic or naphthyl rings with retention of P2YR potency. This broad tolerance for steric bulk in a distal region was not observed for dinucleoside tetraphosphate agonists with both nucleobases substituted. The potent N 4-(3-(4-methoxyphenyl)-propyl)oxy analogue 19 (EC50: P2Y2R, 47 nM; P2Y4R, 23 nM) was functionalized for chain extension using click tethering of fluorophores as prosthetic groups. The BODIPY 630/650 conjugate 28 (MRS4162) exhibited EC50 values of 70, 66, and 23 nM at the hP2Y2/4/6Rs, respectively, and specifically labeled cells expressing the P2Y6R. Thus, an extended N4-(3- arylpropyl)oxy group accessed a structurally permissive region on three G q-coupled P2YRs, and potency and selectivity were modulated by distal structural changes. This freedom of substitution was utilized to design of a pan-agonist fluorescent probe of a subset of uracil nucleotide-activated hP2YRs.
- Jayasekara, P. Suresh,Barrett, Matthew O.,Ball, Christopher B.,Brown, Kyle A.,Hammes, Eva,Balasubramanian, Ramachandran,Harden, T. Kendall,Jacobson, Kenneth A.
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p. 3874 - 3883
(2014/05/20)
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- 1-AZA-BICYCLO [2.2.2] OCTANE DERIVATIVES USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS
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The invention provides named compounds of formula (I), pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions and their use in therapy.
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Page/Page column 73-74
(2010/01/12)
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- MACROLIDE DERIVATIVES
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Compounds represented by formula (I) and the formula (IV) have an inhibitory activity of MMP-9 production, therefore, are useful as a medicine agent with fewer side effects than conventional MMP enzyme activity inhibitors, as a prophylactic and therapeuti
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Page/Page column 56
(2009/04/24)
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- Synthesis and Pharmacology of a Series of 3- and 4-(Phosphonoalkyl)pyridine- and piperidine-2-carboxylic Acids. Potent N-Methyl-D-aspartate Receptor Antagonists
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We recently prepred a series of 3- and 4-(phosphonoalkyl)pyridine- and piperidine-2-carboxylic acids as antagonists of neurotransmission at N-methyl-D-aspartate (NMDA) preferring receptors.NMDA antagonists may prove to be useful therapeutic agents, for instance, as anticonvulsants, in the treatment of neurodegenerative disorders such as Alzheimer's disease and in the prevention of neuronal damage that occurs during cerebral ischemia.The compounds prepared were evaluated for their ability to displace CPP binding (an assay shown to be selective for compounds that bind at the NMDA receptor) and for their ability to block NMDA-induced lethality in mice (an assay that is also specific for competitive and noncompetitive NMDA antagonists).Two of the compounds, cis-4-(phosphonomethyl)piperidine-2-carboxylic acid (11a) and cis-4-(3-phosphonoprop-1-yl)piperidine-2-carboxylic acid (11c) proved to be potent NMDA antagonists. 11a and 11c displaced CPP binding with IC 50's of 95 and 120 nM, respectively, and both protected mice from NMDA-induced lethality, with MEDs (minimum effective dose, the dose at which three of the five animals tested survived) of 10 and 40 mg/kg ip, respectively.The rest of the compounds prepared were weakly active or inactive in these assays.The pattern of activity observed for this series parallels that observed for the acyclic series of ω-phosphono-α-amino acids, where AP5 and AP7 possessed NMDA antagonist activity while AP6 and AP8 were inactive.Reduction of conformational mobility by incorporation of the piperidine ring led to enhanced potency relative to the acyclic analogues.
- Ornstein, Paul L.,Schaus, John M.,Chambers, John W.,Huser, Diane L.,Leander, J. David,et al.
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p. 827 - 833
(2007/10/02)
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