β-Secretase (BACE1) has been broadly documented as one of the possible therapeutic targets for the treatment of Alzheimer’s disease. In this paper, we report the synthesis and the for β-secretase (BACE-1) inhibitory activity of new series of tetrahydrobenzo [b] pyran derivatives. One-pot synt...
Transition metal-catalyzed cross-coupling reactions of arylmetal reagents with ethyl bromodifluoroacetate have been explored. After intensive investigations, we have successfully found that a cobalt-catalyzed cross-coupling reaction (catalytic alkoxycarbonyldifluoromethylation) of arylzinc reage...
The reaction of the equimolar mixture of imidazole and 1,4-butane sultone was performed at 90 °C in ethylbenzene for 12 h, and the structure of the product was investigated by the NMR analysis in CD3OD and DMSO‑d6. This work demonstrated that 4-imidazol-1-yl-butane-1-sulfonic acid could not be ...
The effect of different substituents on the excited state intramolecular proton transfer (ESIPT) of 1-aryl-2-(furan-2-yl)butane-1,3-diones (AYFBD), namely OFBD, TFBD, MFBD and FFBD are studied by employing the density functional theory (DFT) and time-dependent density functional theory (TDDFT) m...
A definitive synthesis of the propyl glycoside (1) of ristotetraose, the heterotetrasaccharide component of the antibiotic ristomycin A (ristocetin A) is described.
Isobutyl palmitate was synthesized by the esterification of palmitic acid and isobutanol with pyridine n-butyl bisulfate ionic liquid as the catalyst in a self-designed reactor. The kinetics of the esterification and cold flow properties of biodiesel were also studied. The optimal reaction condi...
Raman and infrared spectra of n-butyl, isobutyl, sec-butyl and tert-butyl nitrite are reported. Density functional theory and Møeller–Plesset calculations with 6-31G* and 6-311G* basis sets were used to determine ground state molecular geometries and vibrational frequencies of these compounds. ...
The crystal and molecular structures of (Z)-4,4',6-triacetoxy aurone (I) and (Z)-3',5'-di-bromo-2',4,4',6-tetrahydroxyaurone monohydrate (II) have been studied by X-ray analysis and AM1 molecular orbital methods. Aurones are characterized by a methine bridge between the ...
The Rh(II)-catalyzed reaction of 2-carbonyl-substituted 2H-azirines with ethyl 2-cyano-2-diazoacetate or 2-diazo-3,3,3-trifluoropropionate provides an easy access to 2H-1,3-oxazines and 1H-pyrrol-3(2H)-ones. These compounds can be selectively prepared from the same starting material using temper...
Current models imply that the evolutionarily conserved, actin-binding Ezrin-Radixin-Moesin (ERM) proteins perform their activities at the plasma membrane by anchoring membrane proteins to the cortical actin network. Here we show that beside its cytoplasmic functions, the single ERM protein of Dr...
A new class of fluorescent dye which upon excitation at 488 nm turns red is shown to be probe-suitable for using in flow cytometry alone or in conjunction with fluorescein derivatives. 7-dimethylamino 3-(p-formylstyryl) 1,4 benzoxazin 2-one is suitable for rendering microorganisms, such as Plasm...
A suite of nickel, cobalt, iron, copper, and zinc containing sulfides are assayed for the promotion of a model carbon fixation reaction with relevance to local reducing environments of the early Earth. The assay tests the promotion of hydrocarboxylation (the Koch reaction) wherein a carboxylic a...
The Swern oxidation of various benzylic and allylic alcohols, primary alcohols, and secondary alcohols with two ion-supported methyl sulfoxides A-1 (C6) and B-1 (C10), and oxalyl chloride in the presence of triethylamine in dichloromethane, followed by simple diethyl ether extraction of the reac...
Ethylthioalkyl phenylglyoxylates (2) underwent regioselective photocyclization to produce up to 13-membered ring thiacyclols (3) in good yields. Cyclization occurred between the excited carbonyl group and the carbon a to the sulfur on the remote side. The more methylenes placed between the carbo...
Steric and electronic effects in the copper-catalysed asymmetric oxidation of aryl benzyl, aryl alkyl and alkyl benzyl sulfides have been investigated. The presence of an aryl group directly attached to the sulfur is essential to afford sulfoxides with high enantioselectivities, with up to 97% e...
Mo- and Ni-containing carbide catalysts were prepared by a Pechini-based method using citric acid as a complexing agent. All the catalysts were characterized by temperature-programmed reduction, X-ray diffraction (XRD), X-ray photoelectron spectroscopy, and N2 and CO sorption. The XRD experiment...
The effect of 4-week daily administration of 13,14-dihydro-prostaglandin E1 (13,14-DH-PGE1; 2 μg/kg) on LDL influx into the rabbit aortic wall was examined versus the effect of the same dose of PGE1 and sham-treatment in 108 male animals fed an 1% cholesterol supplemented diet. Treatment was st...
ABSTRACTPurposeAlprostadil (prostaglandin E1) is the preferred monotherapy for intracavernous injection in the diagnosis and treatment of erectile dysfunction. Our study was designed to evaluate whether there is a difference in the pharmacokinetics of prostaglandin E1 and its main metabolites af...
The syntheses and characterization of two novel ferrocene derivatives containing 3,5-diphenylpyrazole units of general formula [1-R-3,5-Ph2-(C3N2)-CH2-Fc] {Fc = (η5-C5H5)Fe(η5-C5H4) and R = H (2) or Me (3)} together with a study of their reactivity with palladium(II) and platinum(II) salts or ...
The uptake of styryl phosphoric acid (SPA) by stannic oxide was studied using three independent measures of the adsorption process: (i) adsorption isotherms, (ii) zeta potentials of stannic oxide particles before and after adsorption and (iii) the release of hydroxyl ions from the stannic oxide ...
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