For the first time, derivatives of 3,7-diazabicyclo[3.3.1]nonane (bispidine) were proposed as potential inhibitors of the SARS-CoV-2 main viral protease (3-chymotrypsin-like, 3CLpro). Based on the created pharmacophore model of the active site of the protease, a group of compounds were modeled and tested for activity against 3CLpro. The 3CLpro activity was measured using the fluorogenic substrate Dabcyl-VNSTLQSGLRK(FAM)MA; the efficiency of the proposed approach was confirmed by comparison with literature data for ebselen and disulfiram. The results of the experiments performed with bispidine compounds showed that 14 compounds exhibited activity in the concentration range 1–10 μM, and 3 samples exhibited submicromolar activity. The structure–activity relationship studies showed that the molecules containing a carbonyl group in the ninth position of the bicycle exhibited the maximum activity. Based on the experimental and theoretical results obtained, further directions for the development of this topic were proposed.

The effect of UV radiation on plants provokes oxidative stress, accompanied by the production of reactive oxygen species that can have a direct destructive effect on cellular structures and initiate free radical oxidation of proteins, lipids, and nucleic acids. There is an antioxidant defense system in plant cells that includes a complex of low and high molecular weight compounds. Antioxidants with high molecular weight are enzymes, the key of which is peroxidase [PO]. The paper studies changes in PO activity in soft spring wheat seedlings due to grain treatment with small and medium doses of short-wave UV radiation. A UV-dosed irradiation system (Bio-Link Vilber) with the exposure time 0–60 minutes in increments of 10 minutes was used for seed treatment. Pre-soaked wheat seeds were germinated in Petri dishes. PO activity was determined colorimetrically in three-day-old wheat seedlings, according to A. L. Boyarkin [3]. When the source was irradiated for up to 30 minutes, a clear dependence of the PO activity on the exposure time was not established. The maximum increase in peroxidase activity (by 25.9% relative to the control) was detected with 30-minute UV irradiation. A further increase in exposure time led to a significant decrease in enzyme activity. Moreover, vital feedback was revealed between the activity and exposure time in the range of 30–60 minutes.

No abstract

Проанализирована обращаемость населения г. Барнаула в скорую медицинскую помощь с диагнозом мозговой инсульт в зависимости от типа инсульта, пола, возраста, сезонов года и вариаций солнечной и геомагнитной активности. В соответствии с этим, установлены половозрастные и сезонные особенности развития данного заболевания среди населения г. Барнаула. Выявлено, что обращаемость населения в скорую медицинскую помощь с диагнозом мозговой инсульт связана с повышением уровня солнечной и геомагнитной активности. Наибольшее число обращений населения приходится на период геомагнитных бурь и штормов. При этом развитие мозговых инсультов в ответ на действие факторов геомагнитной активности складывается из немедленных, отсроченных и предшествующих реакций с разными латентными периодами. Barnaul, Russia E-mail: ivbobina@mail.ru Appealability of the population to emergency medical service in Barnaul with the diagnosis of cerebral stroke, depending on type of a stroke, a sex, age, seasons of year and variations of solar and geomagnetic activity is analysed. According to this gender, age and seasonal features of development of the given disease among the population of Barnaul are found. It is revealed that appealability of the population to emergency medical service with the diagnosis of cerebral stroke is bound to rising levels of solar and geomagnetic activity. The greatest number of complaints of the population fall on the period of geomagnetic storms and gales. At the same time development of cerebral strokes in response to action of factors of geomagnetic activity consists of the immediate, delayed and previous response with the different latent periods.

Risk of ischemic events was assessed among 138 men and 184 women on PROCAM Scale. Most of the examined people have risk of ischemic events less than 10%, 17% of men and 21% of women have medium risk, and 6% of men and 11% of women have a high risk. All the examinees with increase of age have a significant increase in the risk of ischemic events. Gender distinctions in risk value are appeared at young age, with aging this difference decreases. At the age of 60 years the risk of ischemic events among representatives of both sexes authentically doesn't differ.