Vol 50, No 4 (2016)

This review addresses progress in the radionuclide diagnosis of oncological diseases using radiopharmaceutical preparations (RPP) based on labeled glucose derivatives. Most attention is paid to 2-[¹⁸F]fluoro-2-deoxy-D-glucose (¹⁸F-FDG), a glucose analog labeled with fluorine-18 (T_1/2 = 110 min) and the only radiotracer for glycolysis, which is used in 90% of clinical studies using positron emission tomography (PET). We describe approaches to the synthesis of ¹⁸F-FDG and state-of-the-art automated technologies allowing tens of clinical doses of RPP for PET investigations of patients to be prepared. The main areas of use of PET with ¹⁸F-FDG in the diagnosis of various tumors are discussed, as is the potential for using glucose derivatives with other radionuclides (⁶⁸Ga, ¹²³I, ^99mTc, ¹⁸⁸Re) as tracers for use in PET and SPECT diagnosis.

A method for preparing the amino, alkoxy, and alkylsulfanyl derivatives of pyrano[4″,3″:4′,5′]pyrido-[3′,2′:4,5]thieno[3,2-d]pyrimidines based on 8-chloro-2,2-dimethyl-5-pyrrolidin-1-yl-1,4-dihydro-2H-pyrano[4″,3″:4′,5′]pyrido[3′,2′:4,5]thieno[3,2-d]pyrimidine was developed. The anticonvulsant activity of the compounds synthesized here was investigated.

A three-component reaction of acetoacetanilides with a mixture of an aromatic aldehyde and thiourea was used to synthesize previously unknown N,6-diaryl-4-methyl-2-thioxo-1,2,3,6-tetrahydropyrimidine-5-carboxamides, which had high analgesic activity and low acute toxicity.

This work was aimed at the synthesis and investigation of the cytotoxic activity of a series of Schiff bases having (4-substituted-benzylidene)-(3-phenyl-1,2,4-oxadiazol-5-yl)methylamine structure with different electronic natures of substituents in the phenyl ring. Thus, the study was intended to observe the effect of substituents with different electronic properties on the cytotoxic activity. The synthesized series of compounds (OP) were obtained by six-step synthesis with yields ranging from 12.23 to 25.77%. The chemical structures of these compounds were elucidated by H NMR. The cytotoxicity of compounds against human oral squamous cell carcinoma cell lines [Ca9-22 (gum), HSC-2 (mouth), HSC-3 (fluent), HSC-4 (language)] and human oral normal cells [HGF (gum fibroblasts), HPC (pulp cells), and HPLF (periodontal ligament fibroblasts)] was tested by MTT assay. Among the group of six OP compounds, bromo derivative OP2, non-substituted derivative OP1, and chloro derivative OP3 showed higher cytotoxicity (2.71-, 1.56-, and 1.53-fold, respectively) than the reference compound 5-FU. In addition, OP2 (3.27) exhibited the greatest selectivity index in this group. These compounds can be considered to be model structures for further studies.

An approach to identifying the effects of different groups of antibiotics (tetracyclines, penicillins, cephalosporins) on the vital activity of lactobacilli by fluorimetry is described. The method is based on measurement of the fluorescence intensity of the intracellular metabolite nicotinamide adenine dinucleotide, reduced form (NADH). Different classes of antibiotics were found to have different effects on lactobacilli. Amoxycillin produced no microbial death, while tetracycline and cephazolin had different levels of fatal effects on lactobacilli.

A new method for assaying the main components of Perftoran formulation based on ¹H and ¹⁹F NMR spectroscopy was developed. The method was developed for inclusion in the Manufacturer’s Pharmacopeia Article for Perftoran.

The diuretic and saluretic activities of aqueous and aqueous-alcoholic extracts of bilberry (Vaccinium myrtillus L.) fruits and shoots were studied in laboratory animals. The results obtained here showed that aqueous extracts of shoots and preparations based on fresh bilberry fruits had moderate diuretic and saluretic activities. Aqueous-alcoholic extracts of air-dried fruits and shoots decreased diuresis and saluresis as compared with a control group.

The processes of preparing film-forming materials based on chitosan with surface modification and ionic cross-linking using sodium tripolyphosphate and potassium pyrophosphate respectively were studied. Optimum cross-linking conditions were identified by studying the interactions of chitosan with different levels of amino group protonation with polyphosphates with different numbers of ionized groups. These studies showed that changes in the duration of treatment of films allowed the level of swelling to be varied over the range 165% to 148% for potassium pyrophosphate and from 196% to 80% for sodium tripolyphosphate. Studies of the kinetics of study drug release showed that changes in the conditions used for modification with polyphosphates could increase the duration of release of the biologically active components to 8 h.

Standard samples constitute one of the key elements in the medicines standardization system. In pharmacopeia analysis in the Russian Federation and many foreign countries, the use of standard samples is regulated by the corresponding normative documents and pharmacopeia monographs. There are different classifications for standard samples and, depending on purpose, certification programs. Standard samples used in compliance with the requirements of pharmacopeia articles or monographs in international, regional and national pharmacopeias are generally termed pharmacopeia standard samples.