R-(–)-1-(Benzofuran-2-yl)-2-propylaminopentane hydrochloride [(–)-BPAP], a highly potent enhancer of impulse propagation-mediated release of catecholamines and serotonin in the brain, and significantly increased the locomotor activity of normal rats at the doses of 0.3 and 1 mg/kg s.c. (P

Dyskinesia consists in a series of trunk, limbs and orofacial involuntary movements that can be observed following long-term pharmacological treatment in some psychotic and neurological disorders such as schizophrenia and Parkinson’s disease, respectively. Agmatine is an endogenous arginine met...

The effect of reserpine on histamine (HA) and tele-methylhistamine (Nτ-MHA) in hypothalamus and cortex of rats was analyzed and compared to catecholamines. IP injection of reserpine (5 mg/kg) confirmed the effectiveness of reserpine treatment on noradrenaline and dopamine levels. Our in-vitro e...

An experimentally simple, efficient, and inexpensive catalyst system was developed for the N-arylation of imidazole, indole, pyrrole, alkyl alcohol amines, and alkyl amines with aryl iodides and bromides. The reaction proceeds in water-ethanol media at 120 °C for 12 h with Cu2O as the catalyst,...

p-Phenyl ethenyl-E-furans (1–6) with varied electron donor and acceptor substituent (NO2, CN, Cl, H, OCH3, NH2) were synthesized and studied the substituent induced optical properties (dipole moment, transition dipole moment, oscillator strength, optical band gap, hyperpolarizability) using Sol...

The regioselective ring-opening reaction of α-methyl-β-propiolactone with 3,3-ethylene-dioxybutylmagnesium bromide in the presence of copper(I) catalyst afforded 2-methyl-6-oxoheptanoic acid, which was easily converted into (E)-3,7-dimethyl-2-2-octene-1,8-diol in good yield.

Monochlorocarbene undergoes addition to bicyclo[2.2.2]octene-2 to give anti- and syn-3-chlorotricyclo[3.2.2.02,4]nonane in a ratio of 5:1. On warming the mixture, only the syn isomer rearranges to 2-chlorobicyclo[3.2.2]nonene-3. The addition of monochlorocarbene to 1-methylnorbomene-2 affords 1-...

To better understand the roles of larger 1-alkenes in reactions leading to the production of polycyclic aromatic hydrocarbons (PAH) and solids in the supercritical pre-combustion environments of future-high-speed-aircraft fuels, supercritical pyrolysis experiments have been conducted with the mo...

Comamonas testosteroni TA441 degrades steroids via 9,17-dioxo-1,2,3,4,10,19-hexanorandrostan-5-oic acid, which is presumed to be further degraded by β-oxidation. In the β-oxidation process, Coenzyme A (CoA)-ester of 9-oxo-1,2,3,4,5,6,10,19-octanor-13,17-secoandrost-8(14)-ene-7,17-dioic acid is...

A 4-pot telescoped procedure to prepare oxetane-3-carboxaldehyde and methyl oxetane-3-carboxylate was developed using readily available starting materials. Classical homologation methods applied to oxetane-3-one proved challenging due to the sensitivity of the oxetane ring toward strongly oxidat...

The synthesis of 1,2,3-triazolo-3′-deoxy-4′-hydroxymethyl carbanucleosides with different reaction conditions and diverse modulations on the heterocycle residues was developed. Heterocycle moieties were efficiently introduced on the pseudo-sugar either via nucleophilic substitution or via 1,3-...

The synthesis of (2RS)-1-(1H-indol-4-yloxy)-3-{[2-(2-methoxyphenoxy)ethyl]amino}propan-2-ol ((RS)-9) and its enantiomers has been described and tested for electrocardiographic, antiarrhythmic, hypotensive and spasmolytic activities as well as for α1-, α2- and β1-adrenoceptors' binding af...

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...

Bazedoxifene is a selective estrogen receptor modulator (SERM) that has been developed for use in post-menopausal osteoporosis. However, it contains a potentially toxic 5-hydroxy-3-methylindole moiety. Previous studies on the 5-hydroxyindole and the 3-alkylindole-containing drugs indometacine, z...

The title compounds were synthesized from the selectively protected N-acylated d-glucosamine derivatives, containing α-halo carboxylic acid moieties, via intramolecular 3-O-alkylation. It was found that if the starting compound contains asymmetric electrophilic center, isomuramic acid derivativ...

1-Piperidino-1-trimethylsilyloxycyclopropane and the corresponding 1-hydroxy-1-piperidinocyclopropane, conveniently prepared from the piperidide of 3-chloropropionic acid, react as cyclopropanone equivalents with various nucleophiles. Use of these derivatives in the formation of pyrroles, pyrrol...

1-Piperidino-1-trimethylsilyloxycyclopropane and the corresponding 1-hydroxy-1-piperidinocyclopropane are conveniently perpared from the piperidide of 3-chloropropionic acid. Reactions of these cyclopropanone equivalents with various nucleophiles are described.

The synthesis, characterization and catalytic performance of chiral Cu(II) complexes derived from N-carboxymethylated and N-carboxyethylated amino acids is reported. The ligand precursors are prepared by single step N-alkylation of the sodium salts of the appropriate chiral amino acid with eithe...

The nickel(II) complexes of formula [Ni(iz)6]X2, (where iz = imidazole, and X = formate, chloroacetate and 2-chloropropionate anions) have been prepared and characterized by spectroscopic methods and magnetic measurements. The crystal and molecular structure of [Ni(iz)6](HCOO)2, 1, [Ni(iz)6](ClC...

The effect of dichloroacetate, an activator of pyruvate dehydrogenase and a hypoglycemic agent, on the oxidation of leucine by the perfused rat heart was studied. Dichloroacetate is known to promote leucine oxidation by liver with the mechanism involving dichloroacetate conversion to glyoxylate ...