The authors have developed a gas chromatographic method for the simultaneous quantification of quazepam in plasma and its two main metabolites, 2-oxoquazepam and N-des-methylquazepam. This method involves an extraction from plasma using butyl acetate, and an analysis by electron-capture detectio...
2-(4-Amino-3-methylphenyl)-5-fluorobenzothiazole (5F 203) and related compounds are a series of anti-cancer candidate pharmaceuticals, that have been shown to activate the AhR. We show that these compounds are high-affinity ligands for the rat AhR, but a quantitative assay for their ability to i...
Effective protocols for the introduction of chiral α-trifluoromethyl benzyl moieties by nucleophilic displacement of enantiomerically enriched α-trifluoromethyl benzylic triflates are presented. The effects of substrate electronics, solvent polarity, temperature, and base are studied by measur...
Experiments were conducted using soybean (Glycine max [L.] Merr. var. “Hobbit”) leaves to measure the effects of selected salicylate derivatives on nitrate and nitrite metabolism. Salicylic acid was previously shown to act as a powerful stimulator of nitrate reduction and a herbicide synergist...
Recent efforts to identify treatments for chronic diabetic complications have resulted in the discovery of a novel series of highly potent and selective (2-arylcarbamoyl-phenoxy)-acetic acid aldose reductase inhibitors. The compound class features a core template that utilizes an intramolecular ...
The tertiary structure of the Leu308Val mutant of human 20α-hydroxysteroid dehydrogenase (AKR1C1) in complex with the inhibitor 3,5-dichlorosalicylic acid (DCL) has been determined. Structures and kinetic properties of the wild-type and mutant enzymes indicate that Leu308 is a selectivity deter...
A series of compounds containing one or two salicylic acid moieties were synthesized, and their efficacy to inhibit the phosphohydrolase activity of PTP1B examined. Some of the methylenedisalicylic acid derivatives were potent inhibitors of PTP1B. Of those derivatives, 3c exhibited about a 14-fo...
A series of pyrrolidinium-based salts with new fluorine-containing anions were synthesized. Different melting points could be obtained by changing the length of the fluoroalkyl chain of the anions. The pyrrolidinium 1,1,2,2-tetrafluoro-2-(1,1,2,2-tetrafluoroethoxy)ethanesulfonate ([C4H8NH2][H(CF...
Treatment of methyl 3,4,6-tri-O-benzyl-2-O-(2,3,4-tri-O-acetyl-α-d-mannopyranosyl)-α-d-mannopyranoside with N,N-diethylaminosulfur trifluoride (Et2NSF3), followed by O-deacetylation and catalytic hydrogenolysis, afforded methyl 2-O-(6-deoxy-6-fluoro-α-d-mannopyranosyl)-α-d-mannopyranoside (8...
(Z)-3-(4-Bromophenyl)-3-(3-pyridyl)allylamine (CPP 200) is transformed to the corresponding chloroimine by hypochlorite ion (ClO−) formed in the presence of myeloperoxidase. A scheme for this transformation is given. The influence of various compounds on this process has been studied. Cysteamine...
By static analytical equilibrium method, the solubilities of 5,10,15,20-tetraphenylporphyrin (TPP) in propionic acid + water solvent mixtures and 5,10,15,20-tetraphenylporphyrin manganese(III) chloride (TPPMnCl) in N,N-dimethylformamide + water solvent mixtures were measured from 303.2 K to 343....
Making use of amide activation, a convenient and short path synthesis of optically pure ω-heterocyclic-β-amino acids has been achieved from (1R,3R)- and (1R,3S)-5-oxo-1-(1-phenyl-ethyl)-pyrrolidine-3-carboxylic acid methyl ester. The key step of the synthesis involves a regiospecific ring-chai...
The presence of small amphiphiles has been found to be necessary in the crystallization of several membrane-protein surfactant complexes. It has been suggested that the role of the small amphiphile may be to reduce the size of the surfactant belt around the protein, making the formation of cryst...
The integral membrane protein CD40 was found on the surface of B lymphocytes that interact with CD40L on T cells during the immune response. The hydrophobic transmembrane domains of membrane proteins can be stabilized in detergent or in lipid bilayers such as liposomes. Membrane proteins can be ...
Carotenoids play an important role in the purple non-sulfur bacteria. In this work we show that addition of the zwitterionic detergent LDAO (lauryldimethylamine N-oxide) to the growth media of Rhodovulum sulfidophilum results in a drastic alteration of the carotenoid biosynthesis, leading to the...
The thermal conductivity of semiclathrate hydrates and aqueous solutions of tetrabutylammonium bromide (TBAB) and tetrabutylammonium chloride (TBAC) was measured for the first time in the temperature range from 223 to 303 K under atmospheric pressure. A transient hot-wire apparatus using a paryl...
Solubility of hydrogen sulfide (H2S) in a new class of solvents, i.e., deep eutectic solvents (DESs) namely, tetrabutylammonium bromide (TBAB)/carboxylic acid and Choline chloride (ChCl)/carboxylic acid, was determined at 298–318 K and 0.10–0.60 MPa. The molar ratio of hydrogen bond acceptor (...
This paper reports the accurate phase equilibrium measurements of two ionic semiclathrate hydrates with tetrabutylammonium bromide (TBAB) and tetrabutylammonium chloride (TBAC). These ionic semiclathrate hydrates are suggested as cool energy storage media for air-conditioning system since their ...
To develop cobalt coating for use in diamond tools, cobalt electrodeposition was conducted in Watts-type baths. The effects of tetrabutylammonium bromide and 2-butyne-1,4-diol on the surface morphology, crystallographic structure, surface roughness and microhardness of thick cobalt deposits were...
Setaria equina heat shock protein (SeqHSP) 70 gene was characterized, cloned and expressed to recombinant protein (rSeqHSP70). The protein was tested for binding with an anti-filarial drug “diethylcarbamazine citrate (DEC)” by equilibrium dialysis method. Molecular docking was also used to det...
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