[QSAR-modeling of desoxyuridine triphosphatase inhibitors in a series of some derivatives of uracil]. / QSAR-modelirovanie ingibitorov dezoksiuridintrifosfatazy v riadu nekotorykh proizvodnykh uratsila.

Due to the widespread prevalence, deoxyuridine triphosphatase (UTPase) is considered by modern biochemists and physicians as a promising target for the development of drugs with a wide range of activities. The therapeutic effect of these drugs will be due to suppression of DNA biosynthesis in various viruses, bacteria and protozoa. In order to rationalize the search for new dUTPase inhibitors, domestic and foreign researchers are actively using the QSAR methodology at the selection stage of hit compounds. However, the practical application of this methodology is impossible without existence of valid QSAR models. With the use of the GUSAR 2013 program, a quantitative analysis of the relationship between the structure and efficacy of 135 dUTPase inhibitors based on uracil derivatives was performed in the IC50 range of 30¸185000 nmol/L. Six statistically significant valid consensus models, characterized by high descriptive ability and moderate prognostic ability on the structures of training and test samples, are constructed. To build valid QSAR models for dUTPase inhibitors can use QNA or MNA descriptors and their combinations in a consensus approach.

["Structure-anti-arrhythmic activity" relationship of N-phenilacetamide derivatives and amides of aromatic carbonic acids].

Using the computer system SARD-21 (Structure Activity Relationship & Design) structural features of high- and low-effective anti-arrhythmic agents have been recognized and the influence of these features on the anti-arrhythmic properties has been evaluated. This information has been used for generation of the model for prediction of anti-arrhythmic effectiveness of pharmaceutical preparations with the 82%-level of recognition by two methods. The recognized structural parameters may be successfully used for design of new highly effective anti-arrhythmic drugs, and also for modification of structures of known anti-arrhythmic drugs for the increase of effectiveness of their anti-arrhythmic action.

[Nonsteroidal anti-inflammatory drugs. Declaration I. A study of interrelation "structure--the effectiveness of anti-inflammatory action"].

Using the computer system SARD-21 (Structure Activity Relationship & Design) the structural features typical for high- and low- effective nonsteroid anti-inflammatory drugs (NSAIDs) were analyzed. This information has been used for the model for prediction of anti-inflammatory effectiveness of medicines with 76% and 81% level of recognition by two methods. New data can be used for creating new highly effective NSAIDs, and for increasing effectiveness of already known components.

[The thromboplastic activity of normal and tumorous human tissues]. / Tromboplasticheskaia aktivnost' normal'nykh i opukholevykh tkanei cheloveka.

The study was made of thromboplastic activity of normal, pathological and tumor human tissues using a hemocoagulatory test-system specifically sensitive to apoprotein III-containing membrane structures. It is established that thromboplastic activity of membrane fragments can be inhibited by native cell components. Blood coagulation and fibrin deposition in tissues can go without cell damaging under initiation by increased permeability of vascular walls and plasma contact with surface of the cells located extravascularly.

[The measurement of NMR-1H relaxation time of blood serum as a method of laboratory diagnosis]. / Izmerenie vremeni IaMR-1H-relaksatsii syvorotki krovi kak metod laboratornoi diagnostiki.

Measurement of NMR-1H-relaxation of the blood serum cannot be employed in the differential diagnosis of individual diseases. This method may be useful as an additional test in examination of the time course of a disease in a patient and in mass screenings or prophylactic check-ups.