The influence of the central hydroxyl groups on the anti-viral activity of symmetrical HIV-1 protease inhibitors derived from l-mannaric acid has been examined. l-Iditol was synthesized and used as a chiral precursor for the synthesis of the corresponding inhibitor with inverted configuration at...

Homogeneous anionic polymerization of 9-(2,3-epoxypropyl)carbazole (EPC) initiated by the complex of 18-crown-6 with potassium hydroxide, potassium acetate or potassium benzoate was carried out in toluene. These catalytic systems allowed polymerization of EPC at low temperature, leading to oligo...

The synthesis of S-(−)-1-(4-(2-ethoxyethoxy)phenoxy)-2-hydroxy-3-(2-(3,4-dimethoxyphenyl)ethylamino)propane hydrochloride (D140S·HCl 6), a novel short acting β1-specific adrenoceptor antagonist, has been described. The antagonist potency for D140S·HCl 6 has been compared with esmolol, another...

The enantioselective synthesis of (−)-syringolides 1 and 2 which were isolated as specific elicitors produced by Pseudomonas syringae pv. tomato was accomplished in 11 steps from diethyl d tartrate. The specific rotations of synthetic samples were in good accord with those of the natural syringo...

The in vitro effect of 4-hydroxylaminoquinoline 1-oxide (4-HAQO) on bacteriophage T4 was investigated. Among five derivatives of 4-nitroquinoline 1-oxide (4-NQO), only 4-hydroxylaminoquinoline 1-oxide produced marked inactivation of the phage.This inactivation effect took place at pH > 7·0 and ...

An Hcr− strain of Bacillus subtilis showed about 10-fold higher sensitivity to killing by 4-hydroxyaminoquinoline 1-oxide (4HAQO) than the parental Hcr+ strain, and the same differential sensitivity was observed between the same pair of strains after UV irradiation or 4-nitroquinoline 1-oxide (4...

In bacteria, 4-nitroquinoline-1-oxide (NQO) causes primarily mutations of the base-substitution type although frameshift mutations are also induced. The adducts formed are presumably recognized by error-prone DNA repair enzymes as evidenced by the much greater activity in plasmid pKM101-bearing ...

In this paper, novel amide-hydroxamic acid surfactants, such as (N-(6-(hydroxyamino)-6-oxohexyl) benzamide (NHOB), N-(6-(hydroxyamino)-6-oxohexyl) octanamide (NHOO), N-(6-(hydroxyamino)-6-oxohexyl) decanamide (NHOD) and N-(4-(hydroxyamino)-4-oxobutyl) octanamide (NOBO), were introduced as flotat...

Oral cancer is one of the most common cancers in the world. Drugs can modulate the expression of drug metabolizing enzymes and are useful in chemoprevention as well as therapy in cancer. 4-Nitroquinoline 1-oxide (4-NQO) is used to induce oral cancer in the present study. In the present investiga...

Neurones in rat hippocampal slices were excited by microiontophoretic applications of N-methyl-D-aspartate (NMDA) and kainate. Responses to NMDA were potentiated by glycine 300 μM or 1 mM in the perfusing medium. A small potentiation of kainate was not observed in the presence of the NMDA antag...

Chronic kynurenine pathway (KP) activation is implicated in Alzheimer's disease (AD) pathophysiology and results in quinolinic acid–induced excitotoxic stimulation of the N-methyl-D-aspartate receptor. However, most studies focus on plasma and it is unclear if peripheral concentrations ref...

α-Deamino-3-(β-d-glucopyranosyloxy)kynurenine, a yellow, fluorescent compound isolated from human lens, was synthesized in 8 steps (10% overall yield) from commercially available 3-methoxy-2-nitrobenzaldehyde. Key events included preparation and glucosylation of methyl 4-(3-hydroxy-2-nitrophen...

Kynurenic acid (KYNA), an antagonist of the α7 nicotinic acetylcholine receptor and the N-methyl-d-aspartate receptor, and 3-hydroxykynurenine (3-HK), a generator of reactive oxygen species, are neuroactive metabolites of the kynurenine pathway of tryptophan degradation. In the mammalian brain ...

SummaryCyclic dinucleotides (CDNs) play key roles as second messengers and signaling molecules in bacteria and metazoans. The newly identified dinucleotide cyclase in Vibrio cholerae (DncV) produces three different CDNs containing two 3′–5′ phosphodiester bonds, and its predominant product is...

The catalysis of 1,2-dibromo-1,2-diphenylethane reduction on platinum and carbon felt electrodes coated by popypyrrole films containing viologen (4,4′-bipyridinium) groups has been investigated. The catalytic activities of polymeric films prepared by electropolymerization of differently substit...

SummaryMeso- and dl-1,2-dibromo-1,2-diphenylethane are both reduced to ∼100% trans-stilbene at the mercury electrode in DMF containing 0.1 M Et4NClO4. Polarographic, coulometric and controlled-potential experiments as well as u.v. spectra substantiate a two-electron process giving the trans-ole...

Both 1,2:5,6-di-O-isopropylidene- and 1,2:5,6-di-O-cyclohexylidene-α-d-glucofuranose-derived ketones provided the corresponding branched 3-C-nitromethyl-congeners in the Henry reaction with nitromethane anion. Reduction of the nitro moiety followed by derivatization with iso(thio)cyanates gave ...

An efficient selective synthesis of C- and O-phosphoryl-substituted phenols from easily available diaryl H-phosphine oxides with quinone monoketals (QMAs) has been developed. With the assistance of opponent characteristic additives (e.g., H2O and Et3N), diaryl H-phosphine oxides could selectivel...

Iodine sorption by polyurethane (PU) and melamine-formaldehyde (MF) foams was studied using both iodine sublimation and iodine solutions with hexanes and toluene. In the sublimation process, the diffusion kinetics was investigated and the interaction between iodine and PU foams was characterized...

With development of personal electronic devices, special energy storage devices such as compressible electrochemical capacitors (CECs) are becoming important. Here, we use artificial melamine sponge (aMS) as matrix, carbon fibers (CFs) as wires to stitch aMS to prepare compressible substrates (a...