The chemistry of N,N′-bisazaheterocycles is gaining importance recently because of their potential role in (1) widening the available pool of chiral auxiliaries in asymmetric synthesis; (2) discovering new molecules as drug candidates; (3) developing organic polymers for use in light harvesting...

Rheological and dielectric behavior of milk/sodium carboxymethylcellulose (Na-CMC) mixtures with 0–10 g/L Na-CMC were investigated from 15 °C to 55 °C. Shear viscosity and viscoelastic behavior of milk/Na-CMC mixtures are mainly controlled by Na-CMC. Raising temperature has an obviously influ...

A series of 2-(methyl-substituted-1H-benzoimidazol-2-yl)-6-(1-aryliminoethyl)pyridines (L1–L6) were synthesized and used as N^N^N tridentate ligands for their nickel complexes (C1–C12). All ligands were fully characterized by elemental, NMR and IR spectroscopic analyses, while their nickel com...

A weakly basic experimental drug, 4-aminopyridine (4-AP), was taken as a model to study the influence of enteric citric acid (ECA) on the release profile from hydroxypropyl methylcellulose (HPMC) matrices, to set up a system bringing about gradual release of the drug. For this purpose, powder mi...

A set of CB2R ligands, based on the thiophene scaffold, was synthesized and evaluated in in vitro assays. Compounds 8c-i, k, l, bearing the 3-carboxylate and 2-(adamantan-1-yl)carboxamido groups together with apolar alkyl/aryl substituents at 5-position or at 4- and 5-positions of the thiophene ...

The neurosteroids allopregnanolone (5α-pregnan-3α-ol-20-one; 5α,3α-P) and its 5β-epimer pregnanolone (5β,3α-P), and pregnenolone sulfate (PS) were examined for effects on spontaneous epileptiform discharges induced by 100 μM picrotoxin (PTX) and 55 μM 4-aminopyridine (4-AP) in the CA3 r...

SummaryThe neurotransmitter glutamate plays a pivotal role in the development of the neuropathological sequelae following acute seizures. Our previous data proved the efficacy of the NMDA-receptor antagonists on the symptoms, survival and neuronal activation in the 4-aminopyridine- (4-AP) induce...

Among different technological variables that influence drug release from hydrophilic matrices, different proportions of the polymer and a water-soluble excipient have been used to control the drug release properties. These variables were used to modify the drug release rate and to examine its ef...

Among different technological variables that influence drug release from hydrophilic matrices, the use of mixtures of polymers represents a potential way of achieving a variety of release properties. Tablets of the model drug 4-aminopyridine with hydroxypropyl methylcellulose were prepared with ...

Cyclodextrins (CDs) were used to increase the aqueous solubility of a recently discovered orally active 3,5-diaryl-2-aminopyridine antimalarial drug lead (MMP). Phase-solubility studies using β-CD, hydroxypropyl-β-CD, and heptakis(2,6-di-O-methyl)-β-CD (DIMEB) as potential solubilizers for MM...

The diastereoselective synthesis of Pro-Phe phosphinyl dipeptide isosteres in protected form was achieved by starting from optically active 1,1-diethoxyethyl(aminomethyl)phosphinate. Our methodology involves diastereoselective α-alkylation and β′-alkylation of phosphinate derivatives with an ...

A variety of physiological functions such as exopolysaccharide synthesis, antibiotic production, and primary metabolism are tightly controlled by quorum sensing in microorganisms. In this study, a marine-derived bacterium Sphingomonas sp. WG was found to possess a cyclo(L-Pro-L-Phe)-mediated quo...

Kinetics and products of the gas-phase reactions of OH radicals with 2-methyl-2-pentanol and 4-methyl-2-pentanol were investigated. Using a relative rate method, rate constants for the gas-phase reactions of OH radicals with 2-methyl-2-pentanol and 4-methyl-2-pentanol of (7.93±0.58)×10−12 cm3 ...

Experimental mole fraction solubilities have been determined for benzoic acid, 4-tert-butylbenzoic acid, 4-chlorobenzoic acid, 2-chloro-5-nitrobenzoic acid, 4-methoxybenzoic acid, salicylamide, 2-ethylanthraquinone, 3,5-dinitrobenzoic acid, 1,4-dichloro-2-nitrobenzene, sorbic acid, 1,4-dibromobe...

An efficient and simple route to biologically and pharmaceutically important o-hydroxyaryl ketones, xanthones, 4-chromanones, and flavones has been developed utilizing readily available carboxylic acids and commercially available o-(trimethylsilyl)aryl triflates.

Some ill-defined carboxylic acids, termed ‘naphthenic acids’ (NA), are best known as important constituents of the > 720 billion litres of process-affected water associated with the expanding oil sands industries. Other NA are components of some immature and biodegraded crude oils and these ma...

We report the synthesis and properties of nucleoside derivatives acylated by 2-(trimethylsilyl)benzoyl (TMSBz) that proved to be extremely stable under basic conditions when introduced into the 5′-hydroxyl group of thymidine, the 4-amino group of deoxycytidine and the 2′-hydroxyl group of urid...

BackgroundThe cytochrome P450 enzyme CYP199A4 can efficiently demethylate 4-methoxybenzoic acid. The substrate is positioned in the enzyme active site with the methoxy group ideally positioned for demethylation. This occurs through interactions of hydrophobic benzene ring with aromatic phenylala...

The paper presents a new method for the determination of 15 carboxylic acids in samples of postoxidative effluents from the production of petroleum bitumens using ion-pair dispersive liquid-liquid microextraction and gas chromatography coupled to mass spectrometry with injection port derivatizat...

A ligand-based virtual screening exercise examining likely bioactive conformations of AM 580 (2) and AGN 193836 (3) was used to identify the novel, less lipophilic RARα agonist 4-(3,5-dichloro-4-ethoxybenzamido)benzoic acid 5, which has good selectivity over the RARβ, and RARγ receptors. Anal...