The isolation of intact long-chain acyl-coenzyme A (acyl Co A) esters is best accomplished by extraction of frozen powdered tissue by the procedure of Mancha et al. [Anal. Biochem. 68 (1975) 600], and the separation of the esters by reverse phase HPLC. The concentration of individual esters iden...
To enhance the solubility and bioavailability of poorly water-soluble Coenzyme Q10 (CoQ10), self-emulsifying drug delivery system (SEDDS) composed of oil, surfactant and cosurfactant for oral administration of CoQ10 was formulated. The solubility of CoQ10 was determined in various oils and surfa...
The terminal enzyme of the linoleoyl-CoA desaturase system was purified from rat liver microsomes by Triton X-100 solubilization, DEAE-cellulose, CM-Sephadex, and affinity chromatography on cytochrome b5-Sepharose. The final enzyme preparation was homogeneous as judged by SDS-polyacrylamide gel ...
The effects of fatty acyl-coenzyme A (CoA) esters (palmitoyl-, stearoyl-, oleoyl-, linoleoyl- and arachidonoyl-CoA) on the synthesis of prostaglandins (PGs) in rabbit kidney medulla microsomes were examined. Medulla microsomes were incubated with arachidonic acid in 0.1 M-TrisHCl buffer (pH 8.0)...
Recent diabetes and obesity research has been focused on the role of intracellular lipids in insulin resistance. Fatty acyl-coenzyme A (CoA) esters play a central role in the trafficking of intracellular lipids, but there has not previously been a method with which to quantify their kinetics usi...
The effects of fatty acyl coenzyme A (CoA) esters (palmitoyl-, stearoyl-, oleoyl-, linoleoyl- and arachidonoyl—CoA) on the activities of lipoxygenase and cyclooxygenase in rabbit platelets were examined. Palmitoyl-, stearoyl-, oleoyl- and linoleoyl- CoA were potent inhibitors of platelet lipoxy...
Exposure to estrogen is associated with increased risk of breast and other types of human cancer. One therapeutic goal would be the creation of new molecules that would retain hormonal potency while incorporating features to retard or prevent quinone toxicity. Hence, new structures closely relat...
A new class of benzoxazole and benzothiazole amide derivatives exhibiting potent CYP3A4 inhibiting properties was identified. Extensive lead optimization was aimed at improving the CYP3A4 inhibitory properties as well as overall ADME profile of these amide derivatives. This led to the identifica...
5-Lipoxygenase (5-LOX) is important enzyme in the biosynthesis of leukotrienes, and is a potential target in the treatment of asthma and allergy. We designed and synthesized a series of benzoxazoles and benzothiazoles as 5-LOX inhibitors. Fourteen compounds prepared showed the inhibition of LTC4...
The vibrational fundamental modes of 2-(methylthio)benzimidazole (2MTBI) have been analysed by combining FTIR, FT-Raman and quantum chemical calculations. The structural parameters of the compound are determined from the optimised geometry by B3LYP with 6-31G∗∗, 6-311++G∗∗ and cc-pVTZ basis sets...
2-Amino-7-substituted benzoxazole analogs were identified by HTS as inhibitors of RSK2. Molecular modeling and medicinal chemistry techniques were employed to explore the SAR for this series with a focus of improving in vitro and target modulation potency and physicochemical properties.
A variety of pyrimidinyl benzoxazoles, benzothiazoles and benzimidazoles linked by thio, methylthio and amino moieties were prepared and studied their antimicrobial and cytotoxic activities. The compound pyrimidinyl bis methylthio benzimidazole 22 was a potent antimicrobial agent particularly ag...
Benzoxazole derivatives, an important type of heterocyclic compounds, have attracted significant interest in photonics and electronics since they are highly efficient luminophores with high photo-stability. The electrochemistry and electrogenerated chemiluminescence (ECL) of benzoxazole derivati...
2-Acetamido-3,4,6-tri-O-acetyl-2-deoxy-α-D-glucopyra-nosyl chloride was condensed with the N-(benzyloxycarbonyl) derivatives of, respectively, L-seryl-glycine ethyl, L-seryl-L-alanine methyl, L-seryl-L-phenylalanine methyl, and L-seryl-L-aspartic dibenzyl esters to give (3-O-GlcpNAc-CbzN-L-Ser)...
The synthesis is described of the glycotripeptide derivatives 2-acetamido-3,4,6-tri-O-acetyl-N-[N-(benzyloxycarbonyl)-L--seryl-L-nitroarginyl-L-aspart-4-oyl]-2-deoxy-β-D-glucopyranosylamine, 2-acetamido-3,4,6-tri-O-acetyl-N-[N-(benzyloxycarbonyl)-L-seryl-L-nitroarginyl-L-aspart-1-oyl-(1-p-nitro...
This chapter provides a comprehensive survey of the literature over the period 1995–2003 of the chemical transformations involved in the synthesis of N-heterosubstituted amides, that is, compounds that contain at least one carbon atom that has one doubly bonded oxygen atom and one singly bonded...
Diiron(II)-(III) complexes [Fe2L(B2](X)2 are prepared, where HL represents 2, 6-bis[bis(2-pyridylmethyl)aminomethyl]-4- methylphenol, HB is carboxylic acid or dicarboxylic acid, and X is ClO4− or BF4−. The valence state of the irons of some complexes is delocalized in the Mössbauer time scale (1...
The selective and efficient solvent-free hydrogenation of bio-based levulinic acid (LA) to γ-valerolactone (GVL) was achieved with new pyridylimine ruthenium(II) complexes as catalyst precursors. The hydrogenation reactions were performed in the presence of formic acid as hydrogen source using ...
Rh-Catalyzed asymmetric 1,4-selective addition of arylboronic acids to β,γ-unsaturated α-keto ester was developed using chiral tert-butanesulfinylphosphine as ligand, good yields (up to 87%), good 1,4-regioselectivities (up to 96:4), and high enantioselectivities (up to 94% ee) were achieved.
The degradation and mineralization of the plant growth regulator 2-(1-naphthyl)acetamide (NAD) was studied by excitation in the presence of the catalyst polyoxometalate decatungstate anion (W10O324−) in aqueous solution under UV (365 nm) or simulated solar light exposure. Our results indicate th...
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