Czech and Slovak Pharmacy, 2006 (vol. 55), issue 3
Original Articles
Synthesis of Reactivators of Phosphorylated Acetylcholinesterase of bis-Pyridiniumdialdoxime Type with a 3-Oxapentane Connecting Chain and Their Testing in vitro on a Model of the Enzyme Inhibited by Chlorpyrifos and Methylchlorpyrifos
K. Musílek, K. Kuča, D. Jun, V. Dohnal, T-H. Kim, Y.-S. Jung, M. Doležal
Čes. slov. farm. 2006, 55(3):115-119 
Insecticides (e. g., parathion, chlorpyrifos, methylchlorpyrifos) and nerve agents (e.g., soman, sarin, tabun, VX) belong to the group of organophosphates. They are able to irreversibly inhibit the enzyme acetylcholinesterase (AChE). Three new reactivators with a 3-oxapentane connecting chain were prepared. The ability of the new compounds to reactivate AChE inhibited by pesticides was tested in vitro and compared to known oximes (pralidoxime, methoxime, trimedoxime, obidoxime, HI-6). The results show that the new substances are superior to known reactivators in the case of methylchlorpyrifos-inhibited AChE at a concentration of 10-3 M which...
Study of a Newly Synthesized Substance with a Potential to Stimulate ß3-Adrenergic Receptors
J. Krčmář, H. Kotolová, L. Veselá, J. Csöllei, T. Goněc, M. Karpíšek, L. Bartošová, J. Nečas
Čes. slov. farm. 2006, 55(3):120-123
ß3-adrenoreceptor agonists can stimulate lipolysis in the white adipose tissue and thermogenesis in the brown adipose tissue. These activities could be useful in the treatment of obesity and the associated metabolic syndrome. The effects of six-week oral administration of the newly synthesized substance B496 (methyl-4-[2-[2-hydroxy-3-(4-ethylcarbamoyl)phenoxyprophyl]amino]etyl)-phenoxyacetate hydrochloride) on serum glucose, triglycerides, total cholesterol, and leptin levels were studied in male Wistar rats fed with a high-fat diet. The animals were divided into a group treated with B496 (5 mg dissolved in 1 litre of water) and a control...
Interconversion of Stereochemically Unstable Chiral Drugs Part III: Using ß-Cyclodextrin as a Chiral Stationary Phase for HPLC Separation of Diazepam Conformers Coupled with an Off-line NMR Experiment
A. Fedurcová, J. Lehotay, T. Liptaj, N. Prónayová, J. Čižmárik
Čes. slov. farm. 2006, 55(3):124-130
Chiral ß-cyclodextrin was used to separate diazepam conformers. Several mobile phases of the composition acetonitrile/acetate buffer 200 mmol/l (pH=3.3, 5.5, 6.5) were employed for this purpose. As follows, the influence of addition of chiral ß-cyclodextrin to the mobile phase on diazepam separation was studied. The interconversion was a concurrence process of separation, resulting from stereolability of the diazepam molecule. The influences of temperature, flow rate, pH, and ionic strength of the mobile phase on interconversion and chromatographic parameters (retention factor and selectivity coefficient) were studied. Complementary off-line NMR measurements...
Analysis of Zinc- and Copper-Containing Tablets in Multicomponent Mineral Nutritional Preparations
A. Planková, O. Štroffeková, E. Havránek
Čes. slov. farm. 2006, 55(3):131-135
The aim of this study was to elaborate and optimize the working conditions for the identification and determination of zinc and copper present in the multicomponent mineral preparations Zinok Walmark® and TrikrátSedem FeCuZn by a modern electrochemical analytical method - galvanostatic stripping chronopotentiometry, and a nuclear analytical method - X-ray fluorescence analysis. The proposed analytical methods were compared with each other and the obtained results concerning the quantity of determined elements were in good agreement.
Review articles
Cytotoxicity Screening and Mode of Action of Natural and Synthetically Prepared Compounds Usable in Tumour Chemotherapy
S. Letašiová, S. Jantová, V. Milata
Čes. slov. farm. 2006, 55(3):99-109
The paper reviews the current approaches to cytotoxic effect screening and mode of action of natural and synthetic compounds usable in tumour chemotherapy. Oncological diseases belong to the most frequently occurring and the most serious diseases that threaten millions of human lives. A serious complication of anticancer therapy is an inadequate therapeutic answer which is caused by the resistance of the human organism to the employed drugs, chemotherapeutic agents. Therefore the resistance is one of the driving forces which constantly force us to search for new anticancer effective drugs of natural or synthetic origin. Primary screening in vitro,...
Present-Day Legislation and the Handling of Chemical Substances and Preparations at the Workplaces Performing Drug Synthesis and Analysis
J. Šubert, Ž. Bezáková
Čes. slov. farm. 2006, 55(3):110-114
The preparation discusses the present-day legislation concerning the handling of chemical substances and preparations in the Czech Republic (Law No. 356/2003 Coll., Regulation No. 369/2005 Coll.), the passages important for the operation of the workplaces performing synthesis and analysis of drugs, including the new duties of the employer. The legal regulation valid in the Czech Republic is compared in the selected parts with that valid in the Slovak Republic. The authors primarily recommend the workplaces engaged in drug synthesis and analysis to limit the use of chemical substances classified as highly toxic.