NOD1 and NOD2 are important members of the pattern recognition receptor family and play a crucial role within the context of innate immunity. However, overactivation of NODs, especially of NOD1, has also been implicated in a number of diseases. Surprisingly, NOD1 remains a virtually unexploited ...

5-Chloro-3-ethyl-N-(4-(piperidin-1-yl)phenethyl)-1H-indole-2-carboxamide (ORG27569, 1) is a prototypical allosteric modulator for the cannabinoid CB1 receptor. Based on this indole-2-carboxamide scaffold, we designed and synthesized novel CB1 allosteric modulators that possess photoactivatable f...

Publisher SummaryIndole is perhaps the single most visible heterocycle in all of chemistry. It is embodied in a myriad of natural products, pharmaceutical agents, and a growing list of polymers. In addition to the hundreds of well-known indole plant alkaloids (e.g. yohimbine, reserpine, strychni...

Prompted by the literature report on anticancer properties of mefenamic acid, a series of mefenamic acid based indole derivatives were designed via a rational approach. Synthesis of this class of compounds was carried out via a 3-step method starting from the mefenamic acid and using the Pd/C–C...

The relative rates at which normal and malignant cells oxidize 4-hydroxycyclophosphamide/aldophosphamide to carboxyphosphamide, a reaction catalyzed by NAD-linked aldehyde dehydrogenases and by aldehyde oxidase, may be potentially important in determining the relative sensitivities of these cell...

Glucokinase (GK) is an enzyme that plays an important role as a glucose sensor while maintaining whole body glucose homeostasis. Allosteric activators of GK (GKAs) have the potential to treat type 2 diabetes mellitus. To identify novel GKAs, a series of compounds based on a thiophenyl-pyrrolidin...

Four cobalt phosphonate coordination polymers Co[(CH3PO3)(H2O)] (1), Co[(C2H5PO3)(H2O)] (2), Co[(C4H9PO3)(H2O)] (3) and Co[(C6H5PO3)(H2O)] (4) have been synthesized using a hydrothermal method. Their crystal structures have been characterized by X-ray diffraction and all exhibit two-dimensional ...

The solvent extraction of zirconium and hafnium from nitric acid solutions into dibutyl butylphosphonate (DBBP)/Solvesso 150 has been studied, as a function of acidity, DBBP and metal concentration. Extraction of complexes containing two DBBP molecules per atom of zirconium or hafnium have been ...

A new pentadecanuclear manganese(II,III) complex derived from tert-butylphosphonic acid with formula [Mn15(μ4-O)6(μ3-O)2(μ2-CH3O)4(CH3O)2(C4H9PO3)10(4-dmbpy)2]·6MeOH (1) (C4H9PO3H2 = tert-butylphosphonic acid, 4-dmbpy = 4,4′-dimethyl-2,2′-dipyridyl) is reported. Complex 1, with an unpreced...

Single crystal and powder EPR studies of VO2+ doped di-ammonium hydrogen citrate [(NH4)2C6H6O7] are carried out at room temperature. The angular variation of the EPR spectra show three different VO2+ complexes that are located in different chemical environment, and each environment contains two ...

Aqueous two-phase systems (ATPS) have been investigated as alternative systems for liquid-liquid extraction. Many ATPS phase diagrams for poly(ethylene glycol) (PEG) have been reported, but little information is available regarding liquid-liquid equilibrium data for poly(propylene glycol) (PPG)....

The Fenton-like reaction of iron(II)-citrate with hydrogen peroxide is physiologically important because it is associated with the oxidative stress and pathological processes induced by the redox-active iron pool in vivo. However, the oxidizing species generated from this reaction at neutral pH ...

Mitochondrial citrate carrier plays a central role in exporting acetyl-CoA in the form of citrate from mitochondria to cytosol thereby connecting carbohydrate catabolism and lipogenesis. In this study, Yarrowia lipolytica mitochondrial citrate carrier was functionally defined and characterized. ...

Incubation of [1-14C]6(Z),9(Z),12(Z)-octadecatrienoic acid with an enzyme preparation from the red alga Lithothamnion corallioidesCrouan led to the formation of two new compounds, i.e. the conjugated tetraene 6(Z),8(E),10(E),12(Z)-octadecatetraenoic acid and the bis-allylic hydroxy acid 11(R)-hy...

A new ST-TTP donor TMEO-ST-TTP, where TMEO-ST-TTP is 2-[4,5-bis(methylthio)-1,3-diselenol-2-ylidene)-5-(4,5-ethylendioxy-l, 3-dithiol-2-ylidene)-l,3,4,6-tetrathiapentalene, has been prepared. It affords highly conducting PF6− and AsF6− salts retaining metallic conductivity down to 4.2 K, while t...

The enthalpies of reaction of 17 alkyl halides with magnesium metal in diethyl ether were measured by use of a steady-state heat flow calorimeter. Enthalpies of formation of the alkyl bromides were determined via the enthalpies of reaction of the alkylmagnesium bromides with hydrogen bromide. Th...

Pd-catalyzed cross-coupling of 2-bromo-3,3,3-trifluoropropene (BTP) and arylmagnesium bromides was investigated. Diphenylphosphinomethane (dppm) was exclusively effective in the coupling among the phosphine ligands tested with Pd(0) and Pd(II) complexes. The use of diphenylphosphinomethane-coord...

The chiral inversion properties of 4-(4-methylphenyl)-2-methylthiomethyl-4-oxobutanoic acid (KE-748), an active metabolite of 2-acetylthiomethyl-4-(4-methylphenyl)-4-oxobutanoic acid (KE-298), were compared with those of ibuprofen in rats. After administration of R(−)-[2α-2H]KE-748, S(+)-KE-748...

The title molecule, N-(5-(4-methylbenzoyl)-2-oxo-4-(4-methylphenyl)pyrimidine-1(2H)-yl)-4-methylbenzamide (C27H23N3O3), was synthesized and characterized by elemental analysis, IR, Raman, 1H and 13C NMR spectral data. To determine conformational flexibility, potential energy surfaces of the titl...

The rearrangement of eight new Z-arylhydrazones of 3-benzoyl-5-phenylisoxazoles (3d–k) into the relevant 2-aryl-4-phenacyl-2H-1,2,3-triazoles (4d–k) in dioxane/water solution at different proton concentrations has been quantitatively studied in a wide temperature range (293–333 K). The data c...