A5110571508- Synthesis and biological activity
- Phenothiazines and Benzothiazines Synthesis and Activities
- Synthesis and Biological Evaluation
- Click Chemistry and Applications
- Bioactive Compounds and Antitumor Agents
- Synthesis of Indole Derivatives
- HIV Research and Treatment
- Bioactive natural compounds
- Synthesis of Organic Compounds
- Synthesis and Reactions of Organic Compounds
- Epigenetics and DNA Methylation
- Cancer-related Molecular Pathways
- Fungal Plant Pathogen Control
- Drug Solubulity and Delivery Systems
- Porphyrin and Phthalocyanine Chemistry
- Diet, Metabolism, and Disease
- Chemical Reaction Mechanisms
- Carbohydrate Chemistry and Synthesis
- Lanthanide and Transition Metal Complexes
- Genomics, phytochemicals, and oxidative stress
- Immunotherapy and Immune Responses
- Analytical Chemistry and Chromatography
- Protein Interaction Studies and Fluorescence Analysis
- Ubiquitin and proteasome pathways
- HIV/AIDS drug development and treatment
Gause Institute of New Antibiotics Russian Academy of Medical Sciences
2005-2025
Institute of Biomedical Chemistry
2018
Russian Academy of Sciences
2016
Novel derivatives of Mycosidine (3,5-substituted thiazolidine-2,4-diones) are synthesized by Knoevenagel condensation and reactions thiazolidines with chloroformates or halo-acetic acid esters. Furthermore, 5-Arylidene-2,4-thiazolidinediones their 2-thioxo analogs containing halogen hydroxy groups di(benzyloxy) substituents in 5-benzylidene moiety tested for antifungal activity vitro. Some the compounds exhibit high activity, both fungistatic fungicidal, lead to morphological changes Candida...
Introduction: A new series of triazoles with antifungal activity have been synthesized in a one-step fashion by direct reaction 2-(2,4-difluorophenyl)-2,3-epoxy- 1-(1H-1,2,4-triazol-1-yl)propane various diamines. Method: Obtained compounds were profiled for biological against pathogenic strains fungi C. albicans and A. niger. Molecular modeling was used to predict binding modes. Result: The lead compound 4 times more active than fluconazole demonstrated wider spectrum activity, inhibiting...
The present review is concerned with the synthesis and structure–activity relationship studies of Arbidol its structural analogues. latter are roughly divided into several unequal parts: indole- benzofuran-based compounds, benzimidazole imidazopyridine bioisosteres ring-expanded quinoline derivatives. Much attention focused on various types antiviral activity above-mentioned congeners, as well parent compound itself. Features metabolic changes also discussed. bibliography includes 166 references.
The wide spread of pathogens resistance requires the development new antimicrobial agents capable overcoming drug resistance. main objective study is to elucidate effect substitutions in tris(1H-indol-3-yl)methylium derivatives on their antibacterial activity and toxicity human cells. A series compounds were synthesized tested. Their vitro was performed 12 bacterial strains, including resistant that clinical isolates or collection strains. cytotoxic determined using an test with HPF-hTERT...
The antimicrobial activity and toxicity of three novel synthetic antibacterial agents containing tris(1H-indol-3-yl)methylium fragment were studied in vitro vivo. All compounds revealed high (minimal inhibitory concentration (MIC) 0.13-1.0 µg/mL) against bacteria that either sensitive or resistant to antibiotics, including multidrug-resistant clinical isolates. derivatives combining with relatively low cytotoxicity human donor fibroblasts HPF-hTERT subjected further testing on mice. In vivo...
Abstract Given the immense significance of p53 restoration for anti-cancer therapy, elucidation mechanisms action p53-activating molecules is utmost importance. Here we report a discovery novel allosteric modulation by small molecules, which an unexpected turn in story. We identified structural element involved regulation, whose targeting RITA, PpIX and licofelone block binding inhibitors, MDM2 MDMX. Deletion mutation analysis followed molecular modeling, key residues S33 S37 targeted RITA...
Given the immense significance of p53 restoration for anti-cancer therapy, elucidation mechanisms action p53-activating molecules is utmost importance. Here we report a discovery novel allosteric modulation by small molecules, which an unexpected turn in story. We identified structural element involved regulation, whose targeting RITA, PpIX and licofelone blocks binding inhibitors, MDM2 MDMX. Deletion mutation analysis followed molecular modelling, key residues S33 S37 targeted RITA PpIX....
The difference in the reactivity of maleimide derivatives is explained by method calculating partial charges on carbon atoms 3-substituted-4-bromomaleimides, as well 3D molecular modeling. influence various substituents electron density studied, and significant role steric factors shown. In case 3- (arylthio)- 4-bromomaleimides most favorable structure devoid obstacles, which may explain high this compound.