Volgograd State Medical University

The novel chemotype, azolo[5',1':2,3]pyrimido[5,4-e]tetrazolo[1,5-c]pyrimidines 12, with promising dual action antiglycating and α-glucosidase inhibiting activities was developed basen on reaction of 6-(tetrazol-5-yl)-7-aminoazolo[1,5-a]pyrimidines 3 with (het)aroyl chlorides. The conditions for this process were optimized to achieve high yields of heterocycles 12 upon mild conditions whereas azido-tetrazole tautomerism was revealed for these products 12 and it was shown that the equilibrium is shifted towards azide tautomer. The obtained azolo[5',1':2,3]pyrimido[5,4-e]tetrazolo[1,5-c]pyrimidines 12 inhibited the glycation reaction in the BSA-glucose assay more strongly than pyridoxamine as a reference compound, which is promising in terms of preventing AGEs assosiated pathologies such as long-term complication of diabetes and cancer. Furthermore, some heterocycles 12 inhibited α-glucosidase in the mid-micromolar range - more effectively than acarbose, with an IC₅₀ 17.52 μM for the lead compound 12k.

Quinone oxidoreductase II (NQO2) is a flavoprotein implicated in reactive oxygen species production which can be considered a potential target for anti-inflammatory drugs. Previously, we demonstrated that 2-oxindole derivatives are effective inhibitors of NQO2. In this work, novel 4/5-substituted 3-arylidene-2-oxindoles were synthesized and their affinity towards NQO2 was assessed in vitro. The obtained compounds activated NQO2 up to 85 %. Some derived NQO2 activators showed anti-inflammatory activity via NLRP3 inflammasome activation in LPS + ATP-stimulated murine macrophages. The obtained compounds were shown to be non-toxic in LDH-assay.

Objective. To compare the effectiveness of various treatment options (percutaneous or transluminal methods, laparoscopic, robotic and open interventions) for blunt abdominal trauma. Material and methods. A systematic review was performed in accordance with PRISMA (2020) and AMSTAR (2017) guidelines. We analyzed non-randomized studies between January 1, 2016 (randomized ones without time limits) and September 10, 2024 in the eLibrary, PubMed and Cochrane library databases. Results. Laparoscopic interventions in stable/stabilized patients with blunt abdominal injuries are accompanied by significantly fewer complications compared to laparotomy. At the same time, there are still insufficient data regarding the advantages of laparoscopy in hemodynamically stable /stabilized patients with spleen injuries. Well-planned researches are needed for other organs. There are insufficient data on percutaneous, transluminal and robotic techniques, as well as results of laparoscopy in hemodynamically unstable patients. Conclusion. Laparoscopic interventions in stable/stabilized patients with blunt abdominal injuries are accompanied by significantly fewer complications compared to laparotomy. Further systematic reviews and meta-analyses based on randomized clinical trials are necessary to obtain higher level of evidence and class of recommendations.