Volume 50, Nº 9 (2016)
- Ano: 2016
- Artigos: 12
- URL: https://journals.rcsi.science/0091-150X/issue/view/15224
Molecular-Biological Problems of Drug Design and Mechanism of Drug Action
Critical Development Needs for Recombinant Blood-Coagulation Factors
Resumo
Critical development needs for recombinant blood-coagulation factors (RBCFs) are reviewed. The production of less immunogenic drugs with suppressed induction of inhibitory antibodies and prolonged therapeutic effects resulting from an increased inactivation threshold is demonstrated to be a major need for designing new RBCF modifications differing in structure and composition from endogenous blood-coagulation factors while retaining their activity.
Article
Pharmacokinetics of the Polyaldehyde Dextran Conjugate with Isonicotinic Acid Hydrazide
Resumo
The pharmacokinetics of the promising antituberculosis drug dextrazide, the conjugate of polyaldehyde dextran with isonicotinic acid hydrazide, were studied using outbred ICR mice. The obtained results were indicative of two-phase dextrazide pharmacokinetics.
Synthesis and Antimicrobial Activity of 4-formylphenyl-N-phenylcarbamates
Resumo
Novel phenylcarbamates with isoxazole, nitrofuran, thiosemicarbazone, isonicotinoylhydrazide, and pyridine moieties were synthesized by [3+2]-cycloaddition and condensation reactions of 4-formylphenyl-N-phenylcarbamate. Their antimicrobial activities against museum strains of Gram-positive bacteria Staphylococcus aureus 209-P and Streptococcus pneumoniae, Gram-negative bacteria E. coli O18 and Pseudomonas aeruginosa 165, and human Micrococcus culture were studied. Derivatives with isoxazole, nitrofuran, and hydrazide moieties were the most active.
New Synthesis and Analgesic and Diuretic Activity of Halo-Substituted 4-Hydroxy-1-Methyl-2,2-Dioxo- 1H-2λ6,1-Benzothiazine-3-Carboxanilides
Resumo
A simple new method for synthesizing N-aryl-4-hydroxy-1-methyl-2,2-dioxo-1H-2λ6,1-benzothiazine-3-carboxamides in high yields is proposed. A series of halo-substituted derivatives were synthesized. Their PMR and 13C NMR spectra and mass spectrometric characteristics were studied. Preliminary pharmacological screening showed that the investigated class of compounds was promising for designing potential analgesics and diuretics, thereby confirming the highly effective “flip-flop drug” methodology.
Antiviral Activity of SIO2–Polyphenol Composites Prepared Mechanochemically from Plant Raw Materials
Resumo
Composites of SiO2 and polyphenols from plant raw materials and model composites based on amorphous SiO2 and dihydroquercetin and pyrocatechol were prepared by solid-state mechanochemistry. Results for the antiviral activities of these composites with respect to herpes simplex virus type 2 (HSV-2) and West Nile virus are presented and compared with those of several chemotherapeutics and chaga (Inonotus obliquus) extract.
Local Anesthetic Activity of a Promising Piperidine Derivative (LAS-54) in Combination with Epinephrine
Resumo
Results from studies of the local anesthetic activity of LAS-54 [4-(benzoyloxy)-3-butoxypiperidinium chloride] (synthesized at the Laboratory of the Chemistry of Synthetic and Natural Drugs, Bekturov Institute of Chemical Sciences) in combination with epinephrine are presented. It was found that joint application of the vasoconstrictor with LAS-54, especially at low concentrations, prolonged infiltration, conduction, and spinal anesthesia.
Selection of Standardization Parameters and Development of Quality Control Methods for Isoleucyl-Tryptophan Dipeptide Coordination Complex with Iron(II) (Timofer)
Resumo
The coordination complex of the dipeptide isoleucyl-tryptophan with Fe(II) possesses immunostimulating activity and is effective for treating iron- and immunodeficiency and pulmonary, rheumatological, and urological diseases. Results are presented from the development of quantitative assays for isoleucyl-tryptophan– Fe(II) using the Fe(II) ion and the tryptophan indole moiety. The standardization parameters of a reference sample, drug substance, and its dosage form are determined.
Method Validation for Anticomplementary Activity of Human Immunoglobulin Drugs
Resumo
Amethod for determining anticomplementary activity of human immunoglobulin (Ig) preparations for i.v. administration by complement fixation test was validated for accuracy, precision (repeatability, intralaboratory precision), limit of quantitation (LOQ), linearity, and analytical domain. The method could be used for quality assessment using the “anticomplementary activity” as part of the pharmaceutical quality examination of human Ig preparations.
Search for New Drugs
Synthesis and Analgesic Activity of 9-Aryl-12-Imino-10,11-Dioxatricyclo[5.3.2.01,6]Dodecane-7,8,8-Tricarbonitriles and 3-Aryl-1,1,2,2-Tetracyanocyclopropanes
Resumo
9-Aryl-12-imino-10,11-dioxatricyclo[5.3.2.01,6]dodecane-7,8,8-tricarbonitriles were synthesized via the reaction of 1-(2-oxocyclohexyl)ethane-1,1,2,2-tetracarbonitrile with aromatic aldehydes. The corresponding 3-aryl-1,1,2,2-tetracyanocyclopropanes were prepared from bromomalononitrile and aromatic aldehydes. The structures of the synthesized compounds were elucidated using IR, PMR, 13C NMR, and mass spectra. The analgesic activity of the synthesized compounds was investigated.
Medicinal Plants
Antioxidant Activity of Medicinal Plants from Southeastern Kazakhstan
Resumo
The antioxidant activity and total contents of phenolic compounds and flavonoids in extracts of several medicinal plants from southeastern Kazakhstan are studied. Antioxidant activity was evaluated in vitro using the cation-radical 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonate) (ABTS•+), the radical 2,2-diphenyl-1-picrylhydrazyl (DPPH•), and the FRAP method. The antioxidant and antiradical activities of the studied plants varied over wide ranges. Extracts of roots and the aerial part of Geranium collinum had the greatest antioxidant and antiradical activity; of Agrimonia asiatica, Alchemilla vulgaris, and Alhagi pseudalhagi, high activity. The antioxidant activities of H2O–EtOH and H2O–Me2CO extracts of G. collinum and A. asiatica showed a reliable correlation with their contents of phenolic compounds.
Drug Synthesis Methods and Manufacturing Technology
Synthesis and Characterization of Poly(DL-Lactic Acid) Nanoparticles Loaded with the Antituberculosis Drug Isoniazid
Resumo
The possibility of creating a new dosage form of the antituberculosis drug isoniazid using nanoparticles of the polymer poly(DL-lactic acid) was studied. It was shown that nanoprecipitation was promising for preparing nanoparticles and loading them with drugs.
Structure of Chemical Compounds, Methods of Analysis and Process Control
Glyceride Composition of Sea Buckthorn Oil from Altai Krai
Resumo
The compositions of sea buckthorn oil (SBO) glycerides in concentrates from various manufacturers in Altai Krai were studied using high-temperature gas chromatography. The effects of the isolation method and raw material composition on the ratio of SBO triglycerides were studied. It was shown that the analysis provided direct differentiation of mono-, di-, and triglycerides and had demonstrable advantages over methods of fatty-acid analysis employing preliminary sample preparation. It was established that the ratio of individual types of SBO glycerides could be a characteristic of the oil production method and the composition of the used raw material.