The estrogen receptors (ERs) are attractive targets in the treatment of breast cancer and the development of receptor-based breast cancer imaging agents for diagnostic use in biomedical imaging technique positron emission tomography (PET). Tetrahydroisoquinoline derivatives are a class of select...

A concise method for the synthesis of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives from α,α′-dibromo-o-xylenes via sequential C-alkylation and N-alkylation of a glycine anion is described.

In this study, a new skin-depigmenting agent, 2,6-dimethoxy-N-(4-methoxyphenyl)benzamide (DMPB), was synthesized using a combination of benzoic acid and aniline. DMPB exhibited significant depigmentation ability on the UV B-induced hyperpigmentation of the brown guinea pig skin. In addition, the...

Several new benzamides 4a–q were synthesized by stirring in pyridine the acid chlorides 3a–q with the appropriate anthranilamide derivatives 2a–g. Some of the synthesized compounds were evaluated for their in vitro antiproliferative activity against a panel of 5 human cell lines (K562 human c...

In the present study, a series of m-(4-morpholinoquinazolin-2-yl)benzamides were designed, synthesized and characterized. The antiproliferative activities of the synthesized compounds were evaluated against two human cell lines (HCT-116 and MCF-7). Compounds with IC50 values below 4 μM were fur...

G-protein-coupled receptor 52 (GPR52) is classified as an orphan Gs-coupled G-protein-coupled receptor. GPR52 cancels dopamine D2 receptor signaling and activates dopamine D1/N-methyl-d-aspartate receptors via intracellular cAMP accumulation. Therefore, GPR52 agonists are expected to alleviate s...

1-Bromo-2-[14C]pinacolone, (CH3)3C14COCH2Br ([14C]BrPin), was prepared from [1-14C]acetyl chloride and tert-butylmagnesium chloride with cuprous chloride catalyst, followed by bromination. It was examined as an active-site directed label for acetylcholinesterase (acetylcholine acetylhydrolase, E...

Five new di-Schiff base nickel(II) complexes (1–5) of salen type ligands were synthesized in-situ by condensation of 3-(dimethylamino)-1-propylamine with 2-hydroxybenzaldehyde, 2-hydroxy-5-methyl benzaldehyde, 2-hydroxy-5-bromo benzaldehyde, 2-hydroxy-5-nitrobenzaldehyde and 2-hydroxy-1-naphtha...

Dimethylamino pyridinium p-bromo-chlorophenolate crystals were grown by slow evaporation solution growth technique. Single crystal X-ray diffraction studies divulge that the composite belongs to monoclinic system with centrosymmetric space group P 2 (1)/c. The unit cell parameters are a = 9.72 Å...

A wide range of 2-arylbenzo[b]furans are synthesized through domino intermolecular C(aryl)–C(alkynyl) bond formation followed by intramolecular C(alkynyl)–O bond forming cyclization via copper(II)-catalyzed coupling of o-iodophenols and aryl terminal acetylenes. This method requires neither ex...

The present study aimed to evaluate the antinociceptive activity (in inflammatory and neuropathic pain models) and gastroprotective effect of the 3,5-diprenyl-4-hydroxyacetophenone (HYDP), isolated from Ageratina pichinchensis. The gastroprotective activity of this plant was previously reported ...

Photodissociation of 2-, 3-, and 4-hydroxyacetophenone (2-, 3-, and 4-HAP) has been studied by analyzing excited-state potential energy surfaces (PES). For that, ab initio CASSCF(12,12)/6–31++G(d,p) calculations of low-lying excited states have been performed. Molecular beam study of photodisso...

In this work we show that the two known polymorphs of 4′-hydroxyacetophenone (form I, monoclinic, P21/c, Z′/Z = 1/4; form II, orthorhombic, P212121, Z′/Z = 2/8) can be clearly distinguished by diffuse reflectance infrared Fourier-transform infrared (DRIFT) spectroscopy. The experimental studi...

The pyrolyses kinetics of 4- and 2-hydroxyacetophenones in the gas phase were determined in a static system, where the reaction vessel was deactivated with allyl bromide, and in the presence of the free radical inhibitor propene when necessary. The working temperature range was 464–485 °C, and...

1.1. The kava-pyrones kawain and dihydromethysticin are constituents of Piper methysticum which exert anticonvulsant, analgesic and anxiolytic properties.2.2. In the present study the effect of these kava-pyrones were tested on field potential changes (fp) induced by omission of the extracellula...

Publisher SummaryPyrido[1,2-a]pyrimidines represent a simple bicyclic ring system that contains a nitrogen-bridgehead condensed pyrimidine moiety. Synthetic methods for these compounds can often be applied to the preparation of similar bi- and polycyclic ring systems. This chapter covers the pri...

To separate the azeotrope of ethanol and ethyl methyl carbonate (EMC) using ionic liquids (ILs), the σ-profiles of imidazolium-based ILs with different anions [BF4]−, [HSO4]−, [PF6]− and [ClO4]− were calculated by the COSMO-SAC model. Based on the analysis results, 1-ethyl-3-methylimidazolium h...

The potentials of phenolic productions from lignin and black liquor (BL) via hydrothermal technology with the aids of alkalis and hydrogen donors were investigated, by conducting batch experiments in micro-tube reactors with 300 °C sub-critical water as the solvent. The results showed that all ...

Tubular carbonate conduits (TCC) represent the termination of fluid plumbing systems in environments of hydrocarbon seepage and play a relevant role in the discharge of methane from sub-seafloor sediments to the water column. However, the biogeochemical reactions and biological activities involv...

For separating the azeotrope of dimethyl carbonate (DMC) and ethanol, four imidazolium-based ionic liquids were selected as extractants. The liquid-liquid equilibrium data for the ternary systems DMC + ethanol + ILs were determined at 298.15 K under pressure of 101.3 kPa. The effect of ILs anion...