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SCRIPTAID ISOSTERES AND THEIR USE IN THERAPY

Compounds of the invention are of the formula (I); wherein: ? is a double bond and X is C; or ? is a single bond and X is N, CH or CQR1; and wherein: n is 1 to 10; R is H or QR1; each R’ is independently selected from H and QR1; each Q is independently selected from a bond, CO, NH, S, SO, SO2 or O; each R1 is independently selected from C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, substituted or unsubstituted aryl or heteroaryl, acyl, C1-C10 cycloalkyl, halogen, C1-C10 alkylaryl or C1-C10 heterocycloalkyl; L is a nitrogen-containing heteroaryl; and W is a zinc-chelating residue; or a pharmaceutically acceptable salt thereof. The compounds are useful in therapy.

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

A new application about (2R,3S,4R,5R)-2,3,4,5-Tetrahydroxy-6-(((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)hexanal

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A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 499-40-1, Name is (2R,3S,4R,5R)-2,3,4,5-Tetrahydroxy-6-(((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)hexanal, molecular formula is C12H22O11. In a Article£¬once mentioned of 499-40-1, Quality Control of: (2R,3S,4R,5R)-2,3,4,5-Tetrahydroxy-6-(((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)hexanal

Extending the family of quinolone antibacterials to new copper derivatives: self-assembly, structural and topological features, catalytic and biological activity

A new series of copper(ii) compounds, [Cu(pef)2(MeOH)] (1), [Cu(pef)(bipyam)Cl] (2), [Cu(pef)(phen)Cl] (3) and [Cu(pef)(bipy)Cl] (4), bearing the quinolone family member pefloxacin (Hpef) were self-assembled in the presence (optional) of N,N?-donor heterocyclic ligands such as 2,2?-bipyridylamine (bipyam), 1,10-phenanthroline (phen), or 2,2?-bipyridine (bipy). The products were fully characterized, including single-crystal X-ray diffraction analysis of 2-4. The structures are extended into 1D (2), 2D (3), or 3D (4) networks via multiple H-bonds between the monocopper(ii) units and guest water and/or methanol molecules; the latter are arranged into different types of water and hybrid water-methanol clusters. The resulting H-bonded networks were classified from a topological viewpoint, revealing diverse topologies that also include an undocumented type. Compounds 2-4 also act as homogeneous catalysts in a model oxidation reaction, namely the mild oxidation of C6-C8 cycloalkanes by H2O2 at 50 C to give cyclic alcohols and ketones. The effects of various reaction parameters (substrate scope, temperature, and loadings of catalyst, cycloalkane, and oxidant) and selectivity features were investigated. Besides, products 1-4 also show remarkable antibacterial activity against four different microorganisms (Escherichia coli, Xanthomonas campestris, Staphylococcus aureus and Bacillus subtilis), which is superior to that of free Hpef. The interaction of the Cu(ii) compounds with calf-thymus DNA was studied suggesting intercalation as the most possible binding mode. Furthermore, the interaction of the obtained copper(ii) derivatives with human/bovine serum albumin was investigated by fluorescence emission spectroscopy and the corresponding albumin-binding constants were established. This study widens a limited family of transition metal pefloxacin derivatives.

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Artificial metalloenzymes derived from bovine beta-lactoglobulin for the asymmetric transfer hydrogenation of an aryl ketone-synthesis, characterization and catalytic activity

A series of diimines derived from saturated and unsaturated fatty acids and including a dipyridylamine (dpa) or a bispyridylmethane (bpm) scaffold as a chelating moiety were synthesized and characterized spectroscopically. Complexation by [LM(mu-Cl)Cl]2 (M = Ru, L = p-cymene; M = Rh, L = Cp*) afforded the monocationic, mononuclear complexes of general formula [LM(N^N)Cl]Cl with N^N being the diimine ligand. Unsurprisingly, these new complexes catalysed the transfer hydrogenation of an activated aromatic ketone, namely 2,2,2-trifluoroacetophenone (TFACP), in water at neutral pH and mild temperature in the presence of formate as a hydrogen donor. The catalytic activity of the complexes expressed as TOF was shown to depend not only on the metal (Ru or Rh) but also on the chelating entity (dpa or bpm) and the length and nature of the lipidic chain tethered to it. Incorporation of the complexes within bovine beta-lactoglobulin (betaLG) as the protein host was studied by circular dichroism and fluorescence spectroscopy and again noticeable differences were observed between the saturated and unsaturated fatty acid derivatives. Eventually, the ability of the protein hybrids to catalyse the transfer hydrogenation of TFACP was demonstrated. Good-to-quantitative conversions in the corresponding alcohol were reached within 72 h with the rhodium(iii) hybrids and the best enantioselectivities (up to 32% ee for the (R)-enantiomer) were measured with the Rh(iii) cofactors derived from palmitic and stearic acids once incorporated into the isoform A of betaLG. This journal is the Partner Organisations 2014.

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A remarkable temperature-dependent, accidental degeneracy of 31P NMR chemical shifts in Ru(II) diphosphine/diimine complexes

Several cis-RuX2((R)-BINAP)(diimine) complexes have been prepared, and many of these exhibit an unusual temperature-dependent, accidental degeneracy of the 31P shifts in their solution NMR spectra.

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Final Thoughts on Chemistry for (2R,3S,4R,5R)-2,3,4,5-Tetrahydroxy-6-(((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)hexanal

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Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments.Introducing a new discovery about 499-40-1, Name is (2R,3S,4R,5R)-2,3,4,5-Tetrahydroxy-6-(((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)hexanal, category: Tetrahydropyrans.

Novel examples of hybrid organic-inorganic solids based on V4 O124 – building blocks

New hybrid organic/inorganic copper oxovanadium compounds of composition [Cu(dpa)2]4V4O12 (1), Cu2(bipy)2V4O12 (2), and Cu2(bipy)2V6O17 (3), which crystallize in the monoclinic 1, 2 and triclinic 3 symmetry, respectively, were obtained by soft hydrothermal routes. The first two structures present isolated [V4O12]4- anionic units, the structure of 3 exhibits the same [V4O12]4- cycles coupled by V2O5 dimeric bridges propagated as an infinite chain along the c-direction 3. For compound 1, the copper(I) centers are bonded to four nitrogen atoms with a distorted tetrahedral geometry. For compounds 2 and 3, the copper(II) centers are square pyramidal with two nitrogen atoms from the neutral diimine ligand and three oxygen atoms from the oxovanadium sub-unit. In all the compounds described herein, the vanadium ions are as V(V), occupying solely tetrahedral sites.

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Topological diversification in metal-organic frameworks: Secondary ligand and metal effects

A series of interesting coordination polymers have been prepared by the combination of a V-shaped 4,4?-oxybis(benzoic acid) (H2oba) and neutral organonitrogen ligands with different metal ions, namely, {[M(oba)(bpe)]¡¤H2O}n [M = Mn (1), Co (2)], [M(oba)(N3)]n [N3 = dipyridin-2-ylamine; M = Cd (3), Cu (4)] and {[Zn(oba)(N5)]¡¤2H2O}n (5) [bpe = 1,2-bis(4-pyridyl)ethene, N5 = bis(pyridin-2-yl)pyridine-2,6-diamine]. The framework structures of these neutral polymeric complexes have been determined by single-crystal X-ray diffraction studies. Compound 1 has a threefold pcu-type network structure. Although 2 has the same ligands and coordination modes as 1, it consists of corrugated 2D layers formed of a series of squares, which allows the sheets to interpenetrate in an unusual 2D?3D parallel fashion. Polymers 3 and 4 exhibit double-helical chains formed by pi-pi stacking interactions from the phenyl rings of the N3 ligands. Compound 5 forms a 2D supramolecular architecture directed by hydrogen bonding between the NH groups of the N5 ligand, the uncoordinated carboxylate oxygens, and the intercalated water molecules. This work markedly indicates that the effect of auxiliary ligands is significant in the construction of these network structures, which are also well regulated by the metal centers. Thermogravimetric analysis (TGA) and XRPD results for compound 1 as well as luminescent properties for compounds 3 and 5 are discussed. Wiley-VCH Verlag GmbH & Co. KGaA, 2009.

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Complexes of copper(I) thiocyanate with monodentate phosphine and pyridine ligands and the P(,N)-donor diphenyl(2-pyridyl)phosphine

Copper(I) thiocyanate derivatives were prepared by the reaction of CuNCS with pyridine (py) and tertiary monophosphine ligands [PR3 in general; in detail: PPh3, triphenylphosphine, P(4-FPh)3, tris(4-fluorophenyl)phosphine)], as well as the potentially bidentate ligand diphenyl(2-pyridyl)phosphine (PPh2py). Mechanochemical methods were used in some cases to investigate stoichieometries that were not easily accessible by conventional solution syntheses. Three forms of the resulting adducts of CuNCS/PR3/py-base (1:3-n:n) stoichiometry-all containing four-coordinate copper(I) atoms and monodentate N-thiocyanate groups-were confirmed crystallographically. Mononuclear arrays are defined for [(PPh2py)3-n(py)nCuNCS], n = 0, 1, 2, the monodentate thiocyanate being N-coordinated in all; two polymorphs are observed for the n = 2 complex, both crystallizing in monoclinic P21 (Z = 2) cells with similar cell dimensions, but with aromatic components eclipsed about the Cu-P bond in the PPh3 complex, and staggered in the PPh2py complex. Bridging thiocyanate groups are found in the 1:1:1 CuNCS/PPh2py/2-methylpyridine (mpy) and P(4-FPh)3/mpy complexes, wherein centrosymmetric dimers with eight-membered central rings are obtained: [(R3P)(mpy)Cu(NCS)2Cu(PR3)(mpy)], as is also the case in the parent 1:2 CuNCS/PPh2py adduct [(pyPh2P)2Cu(NCS)2Cu(PPh2py)2]. For the 1:1:1 CuNCS/P(4-FPh)3/py and PPh3/Brmpy (Brmpy = 3-bromo-4-methylpyridine) adducts, and, likely, CuNCS/PPh2py/py (1:1:1), single-stranded polymers of the form [?Cu(NCS)(PR3)(py-base)(Cu)?](?|?) with linearly bridging NCS ligands were obtained. Some derivatives, representative of all forms, display medium to strong green to blue luminescence when excited with radiation at 365 nm. The 31P CPMAS NMR spectroscopic data clearly differentiate the inequivalent phosphorus positions within each system, showing a wide range of 1J(31P,63/65Cu) values ranging from 965 Hz for [Cu(NCS)(PPh2py)3] to 1540 Hz for dimeric [(4-FPh)3P(mpy)Cu(NCS)2Cu(P(4-FPh)3)(mpy)], reflecting the large variations in the Cu-P bond length.

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Synthesis, characterisation and electrochemical studies of dioxouranium (VI) complexes of dioxolenes with pyridine bases

Mixed ligand complexs of the formulae UO2 (O O) (L-L) (H2O) (2-5) where O O = dioxolenes viz pyrocatechol (2), tert-butylcatechol (3), di-tert-butylcatechol (4) and tetrachlorocatechol (5) and L-L = pyridine (b), bipyridine (c), o-phenanthroline (d) and dipyridylamine (e) have been prepared and characterised by elemental, IR, UV-vis and thermal analyses. Cyclic voltammograms suggest three successive redox responses. The catechol oxidation is highly sensitive to the nature of the substituents. The low energy transition in the visible region is dependent on the nature of the catechol and pyridine base used. This band is assigned to ligand-to-ligand charge transfer (LLCT) transition and is qualitatively assigned as 3b1 (cat) ? pi* (base) transition.

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Unsymmetrical dinuclear cobalt and nickel trimethylacetate complexes

The reaction of the dinuclear complex Co2(mu-OOCCMe 3)2(eta2-OOCCMe3) 2bpy2 (1) with the polymer [Co(OH)n(OOCCMe 3)2-n]x afforded the unsymmetrical dinuclear complex bpyCo2(mu2-O,eta2-OOCCMe 3)(mu2-O,O?-OOCCMe3) 2(eta2-OOCCMe3) (2). The reaction of 2,2?-dipyridylamine with [Co(OH)n(OOCCMe3) 2-n]x gave rise to the analogous complex [(C 5H4N)2NH]Co2(mu2-O, eta2-OOCCMe3)(mu-OOCCMe3) 2(eta2-OOCCMe3) (3). The reaction of complex 1 with Ni4(mu3-OH)2(mu-OOCCMe 3)4(OOCCMe3)2(MeCN) 2[eta2-o-C6H4(NH 2)(NHPh)]2 (4) produced an isostructural heterometallic analog of complex 2 with composition bpyM2(mu2-O, eta2-OOCCMe3)(mu2-O,O?-OOCCMe 3)2(eta2-OOCCMe3) (5) (M = Co, Ni; Co:Ni = 1:1) and the dinuclear heterometallic complex bpy(HOOCCMe 3)M(mu-OH2)(mu-OOCCMe3) 2M(OOCCMe3)2[o-C6H 4(NH2)(NHPh)] (6) (M = Co, Ni; Co:Ni = 0.15:1.85). Compounds 2 and 5 exhibit ferromagnetic spin-spin exchange interactions.

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The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.499-40-1, Name is (2R,3S,4R,5R)-2,3,4,5-Tetrahydroxy-6-(((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)hexanal, molecular formula is C12H22O11. In a Review£¬once mentioned of 499-40-1, Recommanded Product: (2R,3S,4R,5R)-2,3,4,5-Tetrahydroxy-6-(((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)hexanal

Annual survey of organometallic metal cluster chemistry for the year 2002

The synthetic, mechanistic, and structural chemistry of organometallic metal cluster compounds is reviewed for the year 2002.

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