A series of novel 1,3,4-thia(oxa)diazole substituted 2-(2,4-dioxothiazolidine-5-ylidene)-acetamides 3a-c, 4 and 5a-k have been synthesized following the acylation reaction of 2-amino-5-aryl-1,3,4-oxadiazoles, 5-amino-1,3,4-thiadiazole-2-thiol and it’s S-alkylated derivatives with 2-(2,4-dioxothiazolidine-5-ylidene)acetyl chloride in dioxane medium. The functionalization of compounds 3b, 3c, 5d and 5e was carried out on their N3 position under N-alkylation conditions with N-aryl-2-chloroacetamides in DMF/ethanol medium yielded the corresponding 2,4-dioxothiazolidine-3,5-diacetic acid diamides 6a-e and 7a-b. The structures of target compounds were confirmed by using 1H NMR spectroscopy and elemental analysis. The antioxidant activity evaluation in vitro of the synthesized compounds was performed by the method of scavenging effect on 2,2-diphenyl-1-picrylhydrazyl (DPPH) radicals. As a result, the highly active compound 4, namely 2-(2,4-dioxothiazolidin-5-ylidene)-N-(5-mercapto-[1,3,4]thiadiazol-2-yl)acetamide was found to be the most efficient candidate among all compounds with a radical scavenging ability of 88.9%, which was comparable that for ascorbic acid (92.7%). The experimentally calculated IC50 value of 43.1 μM for compound 4 was lower than for ascorbic acid (50.5 μM).

Following the interaction of 2-chloro-N-(5-aryl-1,3,4-oxadiazole-2-yl) acetamides 1a-b with ammonium thiocyanate in dry acetone, the 5-unsubstituted 2-imino-4-thiazolidinones 4a-b have been synthesized. Compounds 4a-b were subsequently utilized in Knoevenagel condensation with aromatic aldehydes or isatin derivatives to synthesize the series of 5-arylidene/isatinylidene substituted 2-(1,3,4-oxadiazol-2-yl)imino-4-thiazolidinones 5a-h and 6a-d. The structures of target compounds were confirmed by using 1H NMR spectroscopy and elemental analysis. Evaluation of anti-cancer activity in
vitro for the synthesized compounds was performed following the National Cancer Institute protocol against leukemia, melanoma, lung, colon, CNS, ovarian, renal, prostate, and breast cancer cell lines. As a result, the most active compound 5a, namely 2-[5-(4-chlorophenyl)-[1,3,4]oxadiazol-2-ylimino]-5-(4-methoxybenzylidene)thiazolidin-4-one was found to be a highly efficient anti-tumor candidate with average logGI50 and logTGI values of -5.19 and -4.09, respectively

The 18 new thiazolo[4,5-b]pyridin-2-one derivatives have been synthesized using alkylation, cyanethylation, hydrolysis, and acylation reactions. The structures of the obtained compounds have been confirmed by 1H NMR spectroscopy, mass spectrometry, and elemental analysis. The study of the in vivo anti-inflammatory activity of the synthesized substances was assessed by using the functional model of carrageenan-induced rat paw edema. The present results of anti-inflammatory activity have shown that the synthesized compounds demonstrated considerable anti-inflammatory effects. Some of them approach or exceed the comparative drug Ibuprofen in terms of activity.

Abstract

Social avoidance in the concept of “avoidance of corrective  emotional experience” is regarded as one of the pathogenetic  factors that aff ect the course and development of mental disorders and increase distress. We conducted a review of studies that studied the role of social avoidance in social anxiety disorder among individuals with or without post-traumatic experience. Inclusion criteria were: 1) subjects were diagnosed with social anxiety disorder; 2) social anxiety disorder and/or post-traumatic stress was a focus of the study; 3) some assessment or review impact of social avoidance was made; 4) subjects were adolescents or adults. The study of the role of avoiding social events as a traumatic trigger and related socially significant factors (stigma, discrimination, living at constant risk, etc.) indicates a correlation between the pathogenesis of social phobia and comorbid symptoms of post-traumatic distress. Managing social avoidance strategies and accepting the conscious experience of social interaction presupposes a person’s readiness to reactflexibly, stay in contact with their emotions and thoughts, and not spend internal resources to get rid of the inner concerns. In our opinion, this will help reduce the perception of social events as a traumatic (retraumatic) factor, reduce clinically significant manifestations of social anxiety and prevent the development of post-traumatic distress. Limitations and implications of these fi ndings for the psychological support and modifying psychotherapeutic interventions of social anxiety disorder are discussed.

ABSTRACT

The aim: To examine the features of experiences of bereavement reactions and the severity of comorbid mental health problems in persons who lost loved ones during the pandemic.

Materials and methods: 191 volunteers aged 18-60 years participated in this study. All participants were tested during 2018-2020. To assess the mental health problems was used International Neuropsychiatric Interview (MINI) and a set of IAPT scales; to the psycho-emotional distress severity associated with loss of loved ones – Inventory of Complicated Grief, with verification of symptoms of complicated grief based on an independent assessment of two experts; and the quality of life satisfaction was assessed by the Quality of Life Enjoyment and Satisfaction Questionnaire, Short Form.

Results: The results show an association between the severity of symptoms of depression, general anxiety, social avoidance, and loss during the pandemic. The level of psychoemotional distress was associated with the experience of bereavement as a traumatic event for a group of participants who experienced loss during the pandemic and, at the same time, before the pandemic was associated with the severity of depression. Regardless of the time of loss, people who demonstrated signs of complicated grief have a more pronounced comorbid psychopathology, a higher level of psycho-emotional distress, and a lower level of satisfaction with life quality.

Conclusions: It has been established that a person’s ability to experience loss as a traumatic experience and grieve during the pandemic is modified with the context of the life situation and reflects those challenges that impose quarantine restrictions