The plasma/serum concentration of 25-hydroxyvitamin D3 [25(OH)D3] is a diagnostic index for vitamin D deficiency/insufficiency, which is associated with a wide range of diseases, such as rickets, cancer and diabetes. We have reported that the derivatization with 4-(4-dimethylaminophenyl)-1,2,4-t...

Polyurethane films were obtained in the solvent-free cycloaliphatic polyaddition process of 4,4′-methylenebis(cyclohexyl isocyanate), poly(ε-caprolactone) diol or poly(oxytetramethylene) glycol and 1,4-butanediol. Chemical structures of the polymers were confirmed by FTIR, NMR and GPC methods....

This is the first report of application of molten ionic liquid (MIL) for the synthesis of heterocyclic polyureas. An inexpensive and readily available MIL, tetrabutylammonium bromide (TBAB) was used for the synthesis of polymers. Therefore, polycondensation of 4-(4-dimethylaminophenyl)-1,2,4-tri...

Direct substitution of 2-benzenesulphonyl cyclic ethers was studied using a variety of carbon nucleophiles. These nucleophiles included organozinc reagents (derived from aryl, vinyl and alkynyl Grignard reagents) or silyl enol ethers, silyl ketene acetals, allylsilanes and trimethylsilylcyanide ...

The μ-opioid receptor (MOR) is the major opioid receptor targeted by most analgesics in clinical use. However, the use of all known MOR agonists is associated with severe adverse effects. We reported that the 1-phenyl-3,6,6-trimethyl-1,5,6,7-tetrahydro-4H-indazol-4-ones are novel opioid recepto...

The reaction of (hetero)aromatic aldehydes or cinnamaldehyde with di-/multi-ethers in the presence of Bu4NI and tert-butyl hydroperoxide generated corresponding α-acyloxy ethers. Reactions between (hetero)aromatic aldehydes or cyclohexanecarbaldehyde with arylalkyl ketones under similar conditi...

The liquid-liquid equilibrium data for the water + propargyl alcohol (PA) + solvents ternary system were measured at 308.2 K under 101.3 kPa, where solvents refer to ethyl acetate, methyl tert-butyl ether, methyl isobutyl carbinol and chloroform. The tie lines were displayed in ternary phase dia...

Nucleophilic N-methyl cyclic ketene-N,X (X=S, O)-acetals can react with electrophilic aryl isocyanates and aryl isothiocyanates to form ‘push–pull’ mono-adducts, di-adducts and spirobicyclic 6/5 ring compounds.

The 1,3-dipolar cycloaddition of azomethine ylides generated in situ from the reaction of isatins or acenaphthylene-1,2-dione and 1,3-thiazolane-4-carboxylic acid to various exocyclic dipolarophiles synthesized from estrone afforded a library of novel C-16 spiro oxindole or acenaphthylene-1-one ...

Rate constants in the pH range 3–9 for formation of the enethiolate product upon hydrolysis of 3,4-dimethylthiazolium ion, a model for the coenzyme thiamin, have been determined by irreversible iodination of the enethiolate at 25°C and ionic strength 1.0 m in aqueous solution. It is concluded ...

Rate constants for C(α)-proton transfer from racemic 2-(1-hydroxyethyl)-3,4-dimethylthi-oazolium ion catalyzed by lyoxide ion and various oxygen-containing and amine buffers were determined by iodination at 25°C and ionic strength 1.0 m in H2O. Thermodynamically unfavorable C(α)-proton transf...

Rate constants for C(α)-proton transfer from racemic 2-(1-hydroxyethyl)thiamin (HET), 2-(1-hydroxyethyl)oxythiamin (oxy-HET), and several 2-(1-hydroxyethyl)-3-R-4-methylthiazolium ions catalyzed by H2O, hydroxide ion, and various oxygen-containing and amine buffers in the pH range 2–9 were det...

Rate constants for C(α)-proton transfer from racemic 2-(1-hydroxyethyl)thiamin (HET), 2-(1-hydroxyethyl)oxythiamin (oxy-HET), and several 2-(1-hydroxyethyl)-3-R-4-methylthiazolium ions catalyzed by H2O, hydroxide ion, and various oxygen-containing and amine buffers in the pH range 2–9 were det...

3-Benzyl-5-imino-4-thioxo-2-imidazolidinones are obtained in good yields by using commercially available starting compounds when, under low temperature conditions, a solution of dry acetonitrile is electrolyzed at a graphite sheet as cathode to produce cyanomethyl anion as EGB, that is further r...

BackgroundPrevious studies have demonstrated that sulfate conjugation is involved in the metabolism of the active metabolite of tramadol, O-desmethyltramadol (O-DMT). The current study aimed to systematically identify the human cytosolic sulfotransferases (SULTs) that are capable of mediating th...

BackgroundWe synthesized (2RS,4R)-2-(2,4-dihydroxyphenyl)thiazolidine-4-carboxylic acid (MHY384) as a potential tyrosinase inhibitor and investigated its antityrosinase activity.

A new 2-substituted thiazolidine-4(R)-carboxylic acid (TCA), 2-glucosamine-TCA (GlcNH2Cys), was synthesized with its antioxidative properties, compared with those of 2 other 2-substituted TCAs, 2-gluco-TCA and 2-galacto-TCA. The GlcNH2Cys showed antioxidative properties of scavenging reactive fr...

Herein we describe the design, synthesis and biological activities of 2-(substituted phenyl)thiazolidine-4-carboxylic acid derivatives as novel tyrosinase inhibitors. The target compounds 2a–2j were designed and synthesized from the structural characteristics of N-phenylthiourea, tyrosinase inh...

The catalytic allylic difluoromethylation of allyl carbonates with (difluoromethyl)zinc reagent, which can be readily prepared via iodine-zinc exchange reaction of difluoroiodomethane with diethylzinc, was achieved by employing copper salt as a catalyst. The difluoromethylation proceeded with no...

Twelve coordination compounds of Mn2+, Fe2+, Co2+, Ni2+, Cu2+ and Zn2+, with mixed organic ligands 5-methylisophthalic acid, 2,2′-bipyridine or phenanthroline, have been hydrothermally synthesised and characterised. The magnetic properties of the Mn2+, Co2+, Ni2+ and Cu2+ compounds have been in...