The CREB (cAMP responsive element binding protein) binding protein (CBP) and its homolog EP300 have emerged as new therapeutic targets for the treatment of cancer and inflammatory diseases. Here we report the identification, optimization and evaluation of 1-(1H-indol-1-yl)ethanone derivatives as...

Quaternary salt analogues based on the DNA minor groove binder and adenine N3 alkylating agent 5-amino-1-(chloromethyl)-1,2-dihydro-3H-benz[e]indole (aminoCBI) show remarkable effects on the body weight of mice (a long-term failure to gain weight relative to matched controls with no loss of appe...

A series of carbamate analogs of besipirdine (HP 749) was synthesized as potential agents with enhanced cholinomimetic properties for the treatment of Alzheimer's disease. Compound 5a (P10358, 1-[3-fluoro-4-pyridinyl)amino]-3-methyl-1H-indol-5-yl methyl carbamate) emerged as a potent, rever...

Type 5 17β-hydroxysteroid dehydrogenase (17β-HSD5), also known as aldo-keto reductase 1C3 (AKR1C3), is a member of the aldo-keto reductase superfamily of enzymes and is expressed in the human prostate. One of the main functions of 17β-HSD5 is to catalyze the conversion of the weak androgen, a...

A simple, specific, and sensitive high-performance liquid chromatographic (HPLC) assay utilizing ultraviolet (UV) detection for the determination of bisnafide in human plasma was developed, validated, and applied to plasma samples from patients undergoing cancer therapy. Plasma samples, containi...

μ-Opioid receptor (MOR) agonists are analgesics used clinically for the treatment of moderate to severe pain, but their use is associated with severe adverse effects such as respiratory depression, constipation, tolerance, dependence, and rewarding effects. In this study, we identified N-({2-[(...

Novel heteroaryl-containing benzamide derivatives were synthesized and screened using an in vitro assay measuring increases in glucose uptake and glucokinase activity stimulated by 10 mM glucose in rat hepatocytes. From a library of synthesized compounds, 3-(4-methanesulfonylphenoxy)-N-[1-(2-met...

Two cascade coupling reactions were developed between N-alkyl(aryl)-N-methacryloyl benzamides and readily available benzyl alcohols or sodium benzenesulfinates. Through a radical cyclization strategy, these one-pot sequential reactions provided two simple and efficient approaches to the synthesi...

A series of N-(2-(1H-imidazol-1-yl)-2-phenylethyl)arylamides were prepared, using an efficient three- to five-step synthesis, and evaluated for their inhibitory activity against human cytochrome P450C24A1 (CYP24A1) hydroxylase. Inhibition ranged from IC50 0.3–72 μM compared with the standard k...

CYP24A1 (25-hydroxyvitamin D-24-hydroxylase) is a useful enzyme target for a range of medical conditions including cancer, cardiovascular and autoimmune disease, which show elevated CYP24A1 levels and corresponding reduction of calcitriol (the biologically active form of vitamin D). A series of ...

A series of novel benzamide-derived compounds was designed, synthesized and pharmacologically evaluated. Among all 37 synthesized compounds, two series were developed with the modulation of the nature, the position of atoms or groups on the benzamide scaffold, but also the nature of the amine gr...

Microbial deracemisation of racemic N-(1-hydroxy-1-phenylethyl)benzamide to give the (R)-enantiomer is described using whole cells of Cunninghamella echinulata NRRL 1384. The deracemisation involves fast highly (S)-selective oxidation followed by slower partially (S)-selective reduction of the i...

Single crystal of γ-glycine, a polymorphic form of glycine, was grown by slow solvent evaporation technique by the additive of lithium bromide. It was grown from the aqueous solution of glycine and lithium bromide in 2:1 M ratio respectively at room temperature. Good quality of γ-glycine singl...

In present work, cobalt substituted M-type barium nanoferrite of composition BaCoxFe12−x O19 with x = 0.4, 0.8 and 1.0 were prepared via a co-precipitation method. After appropriate heat treatments the samples were characterized by X-ray Diffractometer (XRD), Field Emission Scanning Electron Mic...

MXene as two dimensional (2-D) Titanium (III) Carbide (II) (Ti3C2Tx) nanosheets was synthesized and processed by etching bulk MAX phase Titanium (III) Aluminium Carbide (II) (Ti3AlC2) powders in HF solution. This material demonstrated an extraordinary efficiency for the removal of barium from sy...

The thermodynamic behavior of hydrogen bromide in aqueous mixtures of barium bromide as reflected in activity coefficients was studied at temperatures ranging from 278.15 K to 318.15 K at 10 K intervals and at constant ionic strengths ranging from 0.10 mol·kg-1 to 3.0 mol·kg-1. Electromotive-f...

The Solubility, density and refractive index of the formamide(FA)/N-methylformamide(NMF)/N,N-dimethylformamide(DMF) + rubidim bromide/cesium bromide+ water ternary systems were determined at (283.15, 298.15 and 313.15) K. The solubility of the RbBr and CsBr decrease significantly when adding ami...

Barium ferrite encapsulated polythiophene (BaFe12O19/PTh) nanocomposite has been synthesized to analyse electromagnetic interference (EMI) shielding. The morphological analysis of the synthesized composites has been investigated by scanning electron microscopy (SEM), which confirmed the encapsul...

The extension of stripping potentiometry to the electropositive ion barium was investigated using a thin mercury film on a glassy carbon electrode. Barium was detected at low ppm levels in water/ethanol solutions containing tetraethylammonium bromide as electrolyte. Several parameters were inves...

In this paper we present a major advance in the colloidal stabilization of nanoparticles in complex biological media that is one of the ongoing challenges for the usage of nanoparticles in biomedicine. A very common solution is to coat the nanoparticles surfaces with dextran via an electrostatic...