Vol 50, No 1 (2016)

This review provides a brief description of the main structural and functional features of the κ opioid receptor, along with the properties of its agonists and the potential for using these in medicine. Of all the opioid receptor subtypes, κ receptors are the most attractive in terms of creating new drugs with a minimum of side effects. The opioid κ receptor is a member of the superfamily of metabotropic G-protein-coupled receptors. Opioid κ receptors are widely distributed in the CNS and at the periphery. They are involved in numerous physiological processes, including analgesia, regulation of neuroendocrine secretion, water balance, drinking and feeding behavior, autonomic functions, and the mechanisms of learning and memory. Data have been reported on the existence of three subtypes of κopioid receptor, though the molecular properties of only subtype 1 (ê₁) have been studied.

Interaction of 4-amino-5-(2-alkoxyphenyl)-4H-[1,2,4]triazole-3-thiols with substituted phenacyl bromides was used to synthesize 6-(2′-alkoxyphenyl)-3-aryl-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines. Biological studies identified an interaction between chemical structure and antibacterial activity in this series of triazolothiadiazines.

Interaction of 1,4,5-trisubstituted tetrahydropyrrol-2,3-diones with hydrazine hydrate was used to synthesize 3,4-diaryl5-(4-guanidylsulfonylphenyl)-4,6-dihydropyrrolo[3,4-c]pyrazol-6-ones. The antibacterial activity of these compounds was investigated.

A novel series of 2-azetidinones clubbed with quinazolinone was synthesized using anthranilic acid. All the synthesized compounds were evaluated for their antimicrobial activity against two Gram positive bacterial strains (Bacillus subtilis and Staphylococcus aureus), one Gram negative bacterial strain (Escherichia coli) and two fungal strains (Candida albicans and Aspergillus niger). All the synthesized compounds were also screened for their anticancer activity against human breast cancer cell line, MCF-7. Results of antimicrobial and anticancer study indicate that compounds 12 and 5 (IC₅₀ = 49.52 μM) are the most potent antimicrobial and anticancer agents, respectively.

A new technology for synthesis of the immunomodulator drug Kemantane was developed.

The effects of molar substitution of hydroxyethylstarch on the macromolecule mobility in solution were studied by diffusion-ordered NMR spectroscopy (¹H-DOSY) to measure mean self-diffusion coefficients of hydroxyethylstarch with different levels of modification of amylopectin. Molar substitution of hydroxyethylstarch had the opposite effect on macromolecule mobility from that of branching of the polymer chain. Standard samples and medicinal hydroxyethylstarch substances were shown to be nonuniform in terms of the degree of molar substitution. Inclusion of an additional parameter – molar substitution – into regression equations was found to increase the accuracy of measurement of the molecular weight of hydroxyethylstarches using analytical chemistry transport methods.

Methods of extracting polyprenols from Alcea nudiflora and their immunotropic actions were studied. Administration of Alcea nudiflora polyprenols to mice simultaneously with immunization with sheep erythrocytes produced marked stimulation of primary antibody formation, apparent as an increase in the number of antibody-forming cells in the spleen. In addition, there were increases in the cellularity of the central and peripheral organs of immunity, along with increases in blood erythrocyte and leukocyte levels. The immunomodulatory action of Alcea nudiflora polyprenols was seen not only in normal animals, but also in animals with secondary immunodeficiency states developing in acute toxic hepatitis and sublethal irradiation. In terms of activity in these experiments, Alcea nudiflora polyprenols were as active as the known immunostimulatory substance Immunal.

Filtration is one of the methods on which all the world’s chemical-pharmaceutical industries depend. This technological method is used for the sterilization of labile drugs and to provide them with the required properties. As a result of the introduction of strict GMP rules, most current plants use membrane filtration. We review here the main criteria used for selecting material for sterilizing filtration and provide examples of drugs whose manufacture uses this method.

We present an information-analytical review of methods for evaluating the sterility of solid drug formulations. Current normative documentation regulating the quality of parenteral drugs is analyzed and the main limitations of the test method for this indicator are described. The probability of detecting microorganisms depending on the proportion of contaminated units in a batch and the quantity of sample taken for analysis is assessed. Results obtained from analysis of the State Register of Drugs relating to the nomenclature of drugs in solid formulations and their areas of use are presented. The characteristics of tests for individual pharmacological groups of drugs are described.