[Synthesis and antibacterial activity of the new 9-aminoacridine, 10,11-dihydro-5H-dibenzo[b,f]azepine, polyfluoro 5,6-dihydro-1,3,5-oxadiazine derivatives]. / Sintez i issledovanie antibacterial'noi aktivnosti novykh proizvodnykh 9-aminoakridina, 10,11-digidro-5H-dibenzo[b,f]azepina, poliftorirovannykh 5,6-digidro-1,3,5-oksadiazinov.

Screening among 9-aminoacridine, 10,11-dihydro-5H-dibenz[b, f]azepine and polyfluoro 5,6-dihydro-1,3,5-oxadiazine derivatives allowed to isolate compounds with potential antibacterial activity. Schemes of the active compounds synthesis are given. The most important is the estimation of the oxydiazines activity against gram-positive microorganisms including methicillin-resistant staphylococci. Special attention is paid to the activity of iminodibenzyl derivatives against multiresistant gram-negative microorganisms.

[Effect of enalapril maleate on vascular endothelial function and platelet-endothelial interactions in patients with essential hypertension]. / Vliianie terapii énalaprila maleatom na funktsiiu sosudistogo éndoteliia i trombotsitarno-éndotelial'nye vzaimosviazi u bol'nykh gipertonicheskoi bolezn'iu.

AIM: Evaluation of endothelial function and platelet-endothelial interactions in patients with essential hypertension and dynamics of these changes in the course of treatment with enalapril maleate. MATERIALS AND METHODS: The study included 37 patients with essential hypertension and 22 normotensive volunteers. 17 of hypertensive patients received enalapril maleate (enap, KRKA) 5-20 mg/day during the period of 1.5 months. The complex of investigations included: measurement of total plasma cholesteroi, 12-lead ECG, echocardiography, high-resolution ultrasound investigation of brachio-cephalic arteries, evaluation of flow-mediated dilation, measurement of von Willebrand's factor, spontaneous and induced platelet aggregation. RESULTS: Patients with essential hypertension exhibited higher levels of von Willebrand's factor in plasma and degree of spontaneous and induced platelet aggregation as well as lower responses of vessel wall to hemodynamic stimuli compared to normotensive healthy individuals. There was a strong correlation between endothelial function markers and CAD risk factors, elevation of platelet activity. Treatment with enalapril maleate led to a statistically significant decrease of von Willebrand's factor in plasma and ex vivo platelet aggregation whereas flow-mediated dilatation increased. Values of endothelial function markers and platelet activity approached to those of normotensive subjects and these changes were accompanied by a decrease of ECG signs of left ventricular hypertrophy. CONCLUSION: Patients with essential hypertension were found to have compromised endothelial function. However, the degree of endothelial dysfunction depends not on hemodynamic parameters, but on the cumulative effect of CAD risk factors. Treatment with enalapril maleate may lead to normalisation of endothelial function and decrease of platelet activity.

[Effectiveness of pefloxacin in brucellosis]. / Effektivnost' pefloksatsina pri brutselleze.

The clinical efficacy of pefloxacin in the treatment of 51 and 19 patients with acute and subacute brucellosis respectively was studied. It was shown that in a dose of 400 mg twice a day for 15 days pefloxacin provided a rapid regression of the brucellosis clinical signs. By the efficacy it was not inferior to the combination of doxycycline and rifampicin used in the routine doses. Pefloxacin had no toxic action on the function of the liver, kidneys and hematopoietic system. The side effects were minimal. Pefloxacin did not suppress the immunity. By decreasing the activity of the brucellosis process it promoted normalization of the immunological indices.

[Effect of pefloxacin on luminol-dependent chemiluminescence and leukocyte adhesion]. / Vliianie pefloxacin na liuminolzavisimuiu khemiliuminestsentsiiu i adgeziiu leikotsitov.

The in vitro action of pefloxacin on the luminole-dependent chemiluminescence and adherence of polymorphonuclear leukocytes of guinea pigs was studied within a wide range of the concentrations from 0.1 to 100 micrograms/ml. Pefloxacin did not influence the peak values of the chemiluminescence while in concentrations of 0.1 to 10 micrograms/ml it retarded its attenuation. After incubation of the leukocytes in the presence of 100 micrograms/ml of pefloxacin and the subsequent washing out the drug there was observed a decrease in the chemiluminescence. In concentrations of 0.1 to 100 micrograms/ml pefloxacin had no significant effect on the leukocyte adherence.

[Multifactor analysis of the effect of pefloxacin on the dynamics of antibody synthesis to EV vaccine fraction 1 and hemagglutinins]. / Mnogofaktornyi analiz vliianiia pefloksatsina na dinamiku sintez antitel k 1 fraktsii vaktsiny EV i gemaggliutininov.

Multifactor analysis of the effect of pefloxacin on the primary immune response to T-independent bacterial antigen (EV vaccine fraction 1) and to T-dependent cellular antigen (sheep erythrocytes) in mice was carried out with the use of a wide variety of the doses and administration times. It was shown that in the doses corresponding to the average therapeutic ones pefloxacin had no affect on the humoral immune response to the EV vaccine fraction 1 antigens while with the use of the subtherapeutic doses the effect was stimulating. When the doses were higher than the therapeutic ones pefloxacin retarded the antibody formation. The pattern of the dose-time dependence of the pefloxacin effect in regard to the immune response to the T-independent and T-dependent antigens was found to be of various types which could be characteristic of the different action of the drug on the populations of the regulatory lymphocytes and antibody-forming cells.

[Chemotherapeutic effectiveness of pefloxacin in experimental infections]. / Khimioterapevticheskaia éffektivnost' pefloksatsina pri éksperimental'nykh infektsiiakh.

High efficacy of pefloxacin was shown in its study on albino mice with experimental infections such as sepsis, pneumonia and peritonitis. In the effective doses administered orally the drug rapidly arrested the clinical signs of the diseases and provided the sanation of the organs and tissues. The broad antibacterial spectrum of pefloxacin substantiated its efficacy in the treatment of purulent septic processes due to gram-negative and gram-positive pathogens, as well as in the treatment of mixed infections. It is a drug with prolonged action which was confirmed with its prophylactic use. Pefloxacin was efficient in the treatment of infections of various severity.

[Preclinical pharmacokinetics of pefloxacin]. / Doklinicheskaia farmakokinetika pefloksatsina.

The substance and tablets of pefloxacin mesilate manufactured by the Urals Polytechnical University and the National Research Centre of Antibiotics were studied on rats and dogs with the drug oral administration in single and multiple doses equivalent to the human ones. The bioavailability of the drug was good and its blood levels were efficient for a prolonged period (at least 24 hours) after a single oral administration. No cumulation of the antibiotic after its repeated use was observed. The pefloxacin mesilate tablets proved to be fully equivalent to the drug manufactured by Rhone-Poulenc-Rorer (France).