A5024826748- Plant biochemistry and biosynthesis
- Pharmacological Effects of Natural Compounds
- Carbohydrate Chemistry and Synthesis
- Peroxisome Proliferator-Activated Receptors
- Metabolism, Diabetes, and Cancer
- Chemical Synthesis and Analysis
- Computational Drug Discovery Methods
- Diabetes Treatment and Management
- Synthesis and Biological Evaluation
- Click Chemistry and Applications
- Adipose Tissue and Metabolism
- Natural product bioactivities and synthesis
- Synthesis of Organic Compounds
Novosibirsk Institute of Organic Chemistry
2019-2024
Although the incidence and mortality of SARS-CoV-2 infection has been declining during pandemic, problem related to designing novel antiviral drugs that could effectively resist viruses in future remains relevant. As part our continued search for chemical compounds are capable exerting an effect against virus, we studied ability triterpenic acid amides inhibit main protease. Molecular modeling suggested able bind active site protease via non-covalent interactions. The FRET-based enzyme assay...
Natural and synthetic coumarins are often considered privileged scaffolds for obtaining pharmacological agents with hypoglycemic activity. Chemical modification of leads to antidiabetic greater efficacy. In the present work, twenty monoterpene-substituted 7-hydroxycoumarins were synthesized. A new approach using Mitsunobu reaction was shown be effective synthesis target compounds. All synthesized compounds evaluated in an oral glucose tolerance test, two them containing geranyl (-)-myrtenyl...
Dual PPARα/γ agonists can normalize both glucose and lipid metabolism in patients with type 2 diabetes mellitus. The development of such drugs faced the detection various toxic effects phase III clinical trials. However, two this class managed to pass all stages trials, which makes search for new dual promising. In present study, a series dihydrobetulonic acid amides differing length amino-alcohol linker incorporating pharmacophore fragment (S)-2-ethoxy-3-phenylpropanoic were synthesized....
A series of triterpenic acid amides were synthesized incorporating a 2-ethoxy-3-phenylpropanoic pharmacophore fragment. The compounds tested for their ability to improve glycemic control and counter lipid abnormalities in C57BL/6 mice placed on high-fat/high-cholesterol diet. Of all compounds, the dihydrobetulonic derivative (16b) had most pronounced effect decreasing blood glucose levels, total cholesterol (TC), high-density lipoproteins (HDL). All displayed relatively safe profile animal...