UDC 616–093+547.789

Aim. Synthesis, structure determination, in vivo study of anti-inflammatory (anti-exudative) and ulcerogenic activity, estimation of an impact of novel pyrazolin-5-one bearing thiazolidin4-ones on liver function. Methods. Organic synthesis: multicomponent reactions (MCRs), [2+3]-cycloaddition reactions. Spectral methods: IR, LC-MS, 1H NMR. Biological methods: study of anti-cancer activity (NCI NIH, USA) protocol for 3-cell line panel); carrageenin-induced inflammatory paw edema model of white rats, biochemical laboratory tests (ALT, AST, ALP, γ-GGT levels determination); evaluation of ulcerogenic action. Results. The series of novel C-5 and N-3 substituted 2-[(1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl) amino/imino]thiazolidin-4-ones had been synthesized using MCR and [2+3]-cycloaddition reactions as potential biologically active compounds. The results of screening anti-exudative activity revealed that the tested derivatives possess promising anti-inflammatory effect. The SARs were formed and possible mechanisms of their action were discussed. Conclusions. The results presented in paper suggest that the design and synthesis of new pyrazolin-5-on/ thiazolidin-4-one hybrids as potential molecules are an attractive area for the search for novel agents with promising pharmacological properties.
K e y w o r d s: antipyrine, pyrazolin-5-one, thiazolidin-4-one, hybrids, multicomponent reactions, tautomers/rotamers; anticancer/anti-inflammatory activity

UDC [591.4+612.084]:616.716.8 

The research was devoted to the study of the processes of regeneration of the alveolar process of the jaws of experimental animals under the influence of osteotropic drugs. The study was conducted on 50 Wistar rats of herd breeding aged 30 days at the beginning of the experiment. The duration of the experiment was 30 days. The animals were withdrawn from the experiment under thiopental anesthesia, and the jaws were isolated. Excised fragments of jaw bone tissue were fixed in neutral 10 % formalin, decalcified, and embedded in paraffin. The sections were stained with hematoxylin and eosin. The experimental study on animals made it possible to study the effectiveness of the phased application of osteotropic drugs on the processes of local bone resorption. These studies should be taken into account in the development of treatment and prevention complexes for children with osteogenesis disorders.
Key words: rats, experimental research, osteogenesis, complex of preparations, carcinogenic diet.

UDC 616.314-089.5:616.716.4 

The study was dedicated to the improvement of the safety and effectiveness of conduction anesthesia on the mandible using an alternative method of mandibular anesthesia with appropriate anatomical justification and further testing of its clinical effectiveness. The anthropometric parameters of 91 dry anatomical preparations of the adult mandible were studied. Clinical observations were conducted in 440 patients aged 18 to 65 years. A total of 220 anesthetizations were performed using the traditional Inferior Alveolar Block technique and 220 anesthetizations using the Back Low Block technique for the treatment of caries and its complications. According to the results of a comparative evaluation of mandibular anesthesia using the traditional and the proposed methods with the use of standard anesthetic, a greater effectiveness of anesthesia in the Back Low Block technique was proved, as evidenced by an increase in the index of local anesthesia.

UDC 616.314-002:616.8]-053.2

Epidemiological studies show a high prevalence of dental caries among children in Ukraine, ranging from 53.84% to 96.67%. Somatic pathology is a significant risk factor for the onset and development of caries. In Ukraine, the number of children in need of mental development correction is growing. Therefore, our study aimed to investigate the features of dental caries in children with neuropsychiatric disorders. We examined 108 children aged 13-18 years with neuropsychiatric disorders (main group) and 86 practically healthy children (comparison group). The main group consisted of 48 children with mild to moderate mental retardation, 38 children with autism, and 22 children with Down syndrome. We studied the prevalence of caries (in %), caries intensity (CSI) and level of dental care (LDC).
It was found that in children with neuropsychiatric disorders, the prevalence of dental caries is significantly higher than in children in the comparison group and on average is 92.60±2.52% with a caries intensity of 8.56±0.54 teeth, and 75.58±4.63% and CSI = 5.17±0.47 teeth, respectively (p<0.001). It was found that the prevalence of caries was higher in children with Down syndrome than in children with mild mental retardation and autism. The level of dental care for children was analyzed and it was found that children aged 13-15 years, including the comparison group, have an insufficient level of dental care, which is, however, at the age of 16-18 years the level of dental care has significantly improved