Synthesis, X-ray crystal structure, Hirshfeld surface analysis, and molecular docking study of novel inhibitor of hepatitis B: methyl 4-fluoro-3-(morpholinosulfonyl)benzo[b]thiophene-2-carboxylate.

A method of 4-fluoro-3-(morpholinosulfonyl)benzo[b]thiophene-2-carboxylate synthesis has been developed and the electronic and spatial structure of a new biologically active molecule has been studied both theoretically and experimentally. The title compound was crystallized from acetonitrile and the single crystal X-ray analysis has revealed that it exists in a monoclinic P2/c space group, with one molecule in the asymmetric part of the unit cell. Hirshfeld surface analysis was used to study intermolecular interactions in the crystal.

IncobotulinumtoxinA in aesthetics: Russian multidisciplinary expert consensus recommendations.

Background: Although there are various international consensus recommendations on the use of botulinum neurotoxin type A (BoNT/A) in facial aesthetics, there are no global or Russian guidelines on the optimal dose of incobotulinumtoxinA, free from complexing proteins, within specific aesthetic indications. This article reports the outcomes of two expert consensus meetings, conducted to review and analyze efficacy and tolerability data for incobotulinumtoxinA in various facial aesthetic indications and to give expert consensus recommendations to ensure best clinical practice among Russian clinicians.

Methods: Thirteen dermatology and/or plastic surgery experts attended meetings held in Paris, France (November 2013), and Moscow, Russia (March 2014).

[Outpatient care of patients with atherosclerosis obliterans of lower limb arteries].

Results of application of complex treatment of patients with atherosclerosis obliterans of lower limb arteries by means of perfection of an out-patient stage of the surgical help are presented. Rendering assistance in the conditions of surgical branch of city polyclinic makes modern methods of conservative treatment for the overwhelming majority of patients with an obliterating atherosclerosis of arteries of the bottom extremities more accessible, promotes improvement of indicators of safety of extremities and survival rate of patients.

[Prevention of antibiotic-associated diarrhea in children].

One of the most frequent complications of antibiotic therapy is a diarrheal syndrome, which may be related both to the direct toxic effects of antibiotics on the gastrointestinal tract, and the activation of conditionally pathogenic intestinal flora. Particular attention gets to present the problem of C. difficile-infection, which may be the consequence of the development of pseudomembranous colitis in both children and adults.

[Digestive enzyme activities in rats kept on standard or surplus breast-feeding and on low-protein diet directly after weaning].

Activities of digestive enzymes (maltase, alkaline phosphatase, amino peptidase M, and glycyl-L-leucine dipeptidase) in small and large intestine, liver, and kidney were studied in rats of different ages kept in normal (8) and low (3) amounts of pups per litter. The low-protein diet for 10 days at once after weaning was found to change the mass of the organs and their digestive enzyme activities in all studied rat groups. The revealed changes were more prominent in rats kept under conditions of breast-overfeeding.

[Sepsis-induced immune paralysis: pathogenesis, diagnosis, and possible modes of correction].

Recent clinical and experimental studies indicate that the pathogenesis of a septic process in critically ill patients may be divided into two stages: (1) a systemic inflammatory reaction and (2) immune paralysis. Verification of biological markers of both stages is the key point for choosing adequate drug therapy. Immune paralysis virtually shows no clinical symptoms, at the same time this condition can be diagnosed at the earliest stages, by applying a number of laboratory techniques.

Synthesis of heterocyclic compounds possessing the 4H-thieno[3,2-b]pyrrole moiety.

A series of novel heterocyclic combinatorial libraries containing 4H-thieno[3,2-b]pyrrole, thieno[2',3':4,5]-pyrrol[1,2-d][1,2,4]triazine and thieno[2',3':4,5]pyrrolo[1,2-a]pyrazine heterocyclic moieties were obtained by parallel solution-phase synthesis. Key steps include different reactions of initial alkyl 4H-thieno[3,2-b]-pyrrole-5-carboxylates, such as alkylation with alkylating agents; transformation of the carboxylate group into different reactive functionalities, followed by reactions with electrophilic species; intramolecular cyclizations; and amide bond formation. Simple manual techniques for parallel reactions were coupled with easy purification procedures to give high-purity final products.

[Activity of myocardial sympathetic-adrenal system with various volume of viable myocardium in patients with chronic cardiac failure].

Aim: To estimate sympathetic activity in patients with ischemic heart disease (IHD) complicated by chronic cardiac failure (CCF) depending on the volume of viable myocardium measured by dobutamine stress echocardiography (DSE).

Material And Methods: Planar myocardial I-231-MIBG scintigraphy and dobutamine stress echocardiography were made in 16 patients (9 males and 7 females) aged 43-75 years with CCF (NYHA class II-III) and ejection fraction under 35%. The ratio maximal MIBG absorption in the left ventricular myocardium to maximal MIBG absorption in the mediastenum (H/M) and lung (H/L) were estimated.

[Method for determining dopamine and morphine binding sites in lymphocytes from human peripheral blood].

A histochemical method was designed to detect the regions of binding the dopamine and morphine in human peripheral blood lymphocytes. It is based on incubating the suspension of lymphocytes and conjugated dopamine or morphine with bull serum albumin (BSA) marked by horse-radish peroxidase. After incubation, smears are prepared from the lymphocyte suspension, which are stained by diaminobenzidine in the presence of hydrogen peroxide for peroxidase.

[The human body response to factors related to solar activity variations].

The effect of nonstationary solar processes on human organism was studied. Daily measurements of electrical conductivity of 22 biologically active points on human skin, arterial pressure, and pulse frequency of 30 persons were performed, and their subjective sensations were registered. A comparative analysis of the data and variations in environment parameters, such as local A-index, atmospheric pressure, temperature, and indices of cosmic rays indicated a coincidence of their main periods.

[Supravascular laser exposure in combined modality treatment of patients with arteriosclerosis obliterans of blood vessels of lower extremities].

The efficiency of supravascular laser exposure in multiple-modality treatment of patients with atherosclerosis obliterans with distal vascular lesions is demonstrated and the method of noninvasive laser exposure of the lower limbs is validated. Difficulties in the treatment of this category of patients prompted supplementing traditional therapy by supravascular laser exposure in 32 patients. No laser therapy was used in the controls.

[Photo-hemo-correction in the complex treatment of patients with obliterating atherosclerosis of the arteries of the lower limbs].

Based on the assessment of clinical efficiency of the intravascular and percutaneous photomodification of blood with a helium-neon laser in 170 patients the authors have shown that it is expedient to include the photohemocorrection in the medical programs for the I-III degree ischemia.

Induction of antibodies to methadone during methadone maintenance treatment of heroin addicts and its possible clinical implications.

By means of two different types of enzyme-linked immunosorbent assay (ELISA) techniques, antibodies to methadone were detected in blood plasma of heroin addicts on methadone maintenance treatment. In 11-15% of cases immunoglobulin (Ig) M antibodies were detected, while IgG antibodies were observed in 33-40%. At least two types of antibodies to methadone were induced-antibodies with high affinity to methadone and low-affinity antibodies more specific for morphine than for methadone.

[Ventricular late potentials and ventricular arrhythmias in noncoronarogenic myocardial diseases].

Hemodynamic parameters and survival were studied in 48 patients with noncoronarogenic myocardial diseases (NCMD). The examination included high-resolution electrocardiography and Holter monitoring of cardiac rhythm. Deterioration of pump capacity of the heart was associated with high-grade arrhythmias (4B and higher) while ventricular late potentials were more characteristic for patients with severe hemodynamic disorders and, in particular, with dilated cardiomyopathy.

Antibodies to morphine as indicators of chronic morphine intoxication and impaired immune reactivity.

Chronic morphine treatment of rats for 2 and 4 weeks led to an increase in morphine-binding cells in the spleen, despite the general reduction of mononuclear cell content in the spleen and thymus. Simultaneously, serum antibodies to morphine (AbM) in haemagglutination titres 1:20 and higher appeared in 50% and 80% of animals, respectively. Animals with high titres of AbM had much weaker immune response to a thymus-dependent antigen (sheep red blood cells).

[Embolization of the hepatic artery in the treatment of malignant tumors of the liver].

The results of therapeutic hepatic artery embolization (HAE) in 25 patients with malignant unresectable tumors of the liver are discussed. The proximal segments of the hepatic artery were occluded by metal spirals. Thrombosis of the portal vein was accepted as an absolute contraindication for HAE, and a tumor involving more than 50% of the volume of the liver and chronic hepatic insufficiency were considered relative contraindications.

[Re-artelialization of the liver after intravascular occlusion and the possibilities of re-embolization of the arterial bed of the liver].

Angiographic examinations were performed in 52 patients with portal cirrhosis and 6 patients with tumours of the liver in remote terms (1.5-38 months) after embolization of the hepatic artery. In 20 patients (34.

[Type of behavior and superoxide dismutase activity in the brain of rats (a comparison of 2 Tryon strains)].

Differences in the type of behaviour in capable ("maze-bright") and incapable ("maze-dull") Tryon rats have been demonstrated in the situation with pain-irritated partner by the method of "emotional resonance". Most "bright" rats belonged to the type not avoiding the signals of another pain-irritated rat, they revealed a persistent ecologically defensive reaction of preferring a small closed space. The type of anxiety behaviour prevailed in the group of "dull" rats.

[Spiral coils for arterial occlusion].

Roentgen endovascular occlusion with spiral emboli was used in 240 patients with different diseases. The introduction of spiral emboli into the arteries of abdominal and retroperitoneal organs was fulfilled through usual angiographic catheters. Duration of the arterial occlusion was checked up in the following angiographic examinations and showed the devices described to be appropriate for a continuous arterial blockade.