Pharmaceutical Chemistry Journal (v.45, #11)

Effects of nitrosyl complexes of iron with functional S-ligands on the activity of hydrolytic enzymes by L. V. Tat’yanenko; O. V. Dobrokhotova; I. Yu. Pikhteleva; D. A. Poletaeva; A. I. Kotel’nikov; T. N. Rudneva; N. A. Sanina; S. M. Aldoshin (651-654).
We report here our studies of new nitrosyl complexes of iron of the cationic type - [Fe2(SR′)2(NO)4]2+ with R′ = cysteamine and penicillamine - and of the neutral type - [Fe2(SR″)2(NO)4]0 with R″ = benzthiazoline – on the enzymatic activity of hydrolases – cyclic guanosine monophosphate phosphodiesterase (PDEcGMP) and sarcoplasmic reticulum Ca2+-Mg2+-dependent ATPase (SR-Ca2+-ATPase). All the complexes studied were found to be modulators of both enzymes. They produced weak inhibition of PDEcGMP activity and marked inhibition of active transport by SR Ca2+-ATPase. While having virtually no effect on the hydrolytic center of SR Ca2+-ATPase, the active transport of calcium was completely blocked over the concentration range 1 μM – 0.1 mM, with uncoupling of the hydrolytic and transport functions of this enzyme. This suggests that these complexes can induce structural-functional changes in SR Ca2+-ATPase at concentrations corresponding to an enzyme:inhibitor ratio of 1:1, which is consistent with the antimetastatic action of these compounds.
Keywords: cGMP phosphodiesterase; sarcoplasmic reticulum Ca2+-ATPase; inhibition; sulfur-nitrosyl iron complexes

Synthesis and antiviral activity of 1,2,4-triazine derivatives by V. L. Rusinov; I. N. Egorov; O. N. Chupakhin; E. F. Belanov; N. I. Bormotov; O. A. Serova (655-659).
Interaction of 3-aryl-1,2,4-triazin-5(4H)-ones with indole and its methyl derivative in the presence of N-substituted amino acids activated with dicyclohexylcarbodiimide or ethyl chloroformate led to the formation of 1-acyl-6-indolyl-3-phenyl-1,6-dihydro-1,2,4-triazin-5(4H)-ones. The cytotoxic and antiviral actions of the 12 resulting compounds were studied using vaccinia virus.
Keywords: 1,2,4-Triazines; indoles; naproxen; antiviral activity; amino acids

Synthesis and analgesic activity of the products of the interaction between 3-aroylpyrrolo[1,2-a]-quinoxaline-1,2,4(5H)-triones with benzoic acid hydrazides by I. V. Mashevskaya; R. R. Makhmudov; L. V. Kuslina; I. G. Mokrushin; S. N. Shurov; A. N. Maslivets (660-663).
The synthesis, properties, structure, and analgesic activities of the products of the interaction of 3-aroylpyrrolo[1,2-a]quinoxaline-1,2,4(5H)-triones with benzoic acid hydrazides are described. The significance of the structure-function relationship is discussed.
Keywords: Pyrroloquinoxaline triones; benzoic acid hydrazides; analgesic activity

Synthesis and antifungal activity of monoterpenoids of the carane series by L. E. Nikitina; V. A. Startseva; N. P. Artemova; L. Yu. Dorofeeva; I. V. Kuznetsov; S. A. Lisovskaya; N. P. Glushko; M. P. Kutyreva (664-667).
The antifungal activity of terpenoids of the carane series was studied; an interaction was found between the structures of these compounds and their antifungal properties. The actions of several terpenoids on the adhesive activity and enzyme systems of the fungus Candida albicans were studied.
Keywords: Terpenoids of the carane series; antifungal activity

Synthesis and antimicrobial activity of urea derivatives of (1S,2S)-2-AMINO-1-(4-nitrophenyl)-1,3-propanediol by M. Madesclaire; S. Kh. Sharipova; A. V. Lyamin; A. A. Osipova; E. A. Botkin; Yu. V. Zaitseva; V. P. Zaitsev (668-670).
A series of urea derivatives were synthesized from (1S,2S)-2-amino-1-(4-nitrophenyl)-1,3-propanediol and their antimicrobial activity was studied. The compounds synthesized here showed the greatest levels of activity against strains of Bacillus cereus, Staphylococcus aureus, and Streptococcus haemolyticus.
Keywords: (1S,2S)-2-amino-1-(4-nitrophenyl)-1,3-propanediol; ureas; antimicrobial activity

The effects of different extractants and extraction regimes on the practical yields of total β-carbonyl alkaloids from raw material from Elaeagnus angustifolia L., E. multiflora Thunb., and E. argentea Pursh. were studied. An extractant - a mixture of solvents with different polarities, i.e., chloroform and ethanol - was selected and the optimum extraction conditions were identified: an extraction temperature of 40°C, a loading density of (ρ) of 0.5 g/cm3, a grinding level (D) of 1 – 3 mm, and a raw material:extractant ratio (m c:m e) of 1:30 by weight. These results lead to the possibility of exhaustive extraction of alkaloids from raw material from Elaeagnus L.
Keywords: Extractants; β-carbonyl alkaloids; Eleagnus ; oleaster

Development of extraction techniques and standardization methods for a common lady’s mantle (Alchemilla Vulgaris) extract by I. M. Smolyakova; V. Yu. Andreeva; G. I. Kalinkina; S. N. Avdeenko; P. P. Shchetinin (675-678).
A rational technique for preparing an extract of common lady’s mantle (Alchemilla vulgaris) by multistage countercurrent extraction is described, along with a method for standardizing the extract in relation to flavonoids.
Keywords: Common lady’s mantle (Alchemilla vulgaris); liquid extract; standardization method; flavonoids

A review of the literature from 1957 to 2009 on studies of the interaction of penicillin and cephalosporin antibiotics with metal cations and studies of the structure and properties of the resulting complexes is presented.
Keywords: Metal complexes of penicillins; metal complexes of cephalosporins; beta-lactam antibiotics.

DART mass spectrometry: rapid analysis of soft medicinal formulations by E. S. Chernetsova; R. A. Abramovich; I. A. Revel’skii (698-700).
The possibility of using the DART mass spectrometry method for rapid analysis of soft medicinal formulations is considered. Studies of “tetracycline”, “Sintomycin Liniment”, and “Levomecol” creams and suppositories based on hard fat were studied. The possibility of using this method for the rapid screening of medicinal formulations in search of counterfeits is discussed. This is the first report of the analysis of suppositories using DART mass spectrometry.
Keywords: DART mass spectrometry; rapid screening of medicines for counterfeits; soft medicinal formulations

Studies of the stability of cardiocyclide in substance and a solid dosage form by HPLC by M. S. Sergeeva; L. N. Grushevskaya; N. I. Avdyunina; B. M. Pyatin (701-704).
The aim of the present work was to assess the specificity of an HPLC method developed for analysis of the purity of cardiocyclide within the framework of a study of the stability of cardiocyclide as substance and as a solid dosage formulation. Studies were performed using a liquid chromatograph with a spectrophotometric detector at a wavelength of 210 nm with a linear gradient using two mobile phases (MP): 0.02 M phosphate buffer pH 3.3 (MP A) and a mixture of acetonitrile, methanol, and 0.02 Mphosphate buffer pH 3.3 (50:50:20) (MP B). The gradient regime was: MP A/MP B from 35:65 to 0:100 over 15 min. The chromatography column was of size 150 × 4.6 mm, the sorbent was Luna C18(2), particle size 5 μm. This HPLC method allowed separation of cardiocyclide and its most likely contaminants - the intermediate products of the last two synthesis stages, some of which are also products of hydrolysis, as well as a series of unidentified contaminants in substance and the solid dosage formulation as released. The method also allows other contaminants to be detected, i.e., cardiocyclide degradation products forming on exposure to aggressive environmental factors. The method thus yields data on the stability of the substance and medicinal formulation both at the preparation stages and after incorrect storage.
Keywords: Cardiocyclide; stability; HPLC