A5012805487- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Tuberculosis Research and Epidemiology
- Cancer therapeutics and mechanisms
- Fluorine in Organic Chemistry
- Crystallography and molecular interactions
- Biochemical and Molecular Research
- Synthesis and biological activity
- Epigenetics and DNA Methylation
- Synthesis and Characterization of Pyrroles
- Quinazolinone synthesis and applications
- Asymmetric Synthesis and Catalysis
- Synthesis and Biological Evaluation
- Pneumocystis jirovecii pneumonia detection and treatment
- Cyclopropane Reaction Mechanisms
- Genetics, Bioinformatics, and Biomedical Research
- Carbohydrate Chemistry and Synthesis
- Synthesis and Characterization of Heterocyclic Compounds
- Synthesis and Reactions of Organic Compounds
National Academy of Sciences of Ukraine
2018-2021
Institute of Bioorganic Chemistry and Petrochemistry V.P. Kukhar
2020-2021
University of Antwerp
2016-2020
GlaxoSmithKline (Spain)
2016-2020
In this study, a new series of more than 60 quinoline derivatives has been synthesized and evaluated against Mycobacterium tuberculosis (H37Rv). Apart from the SAR exploration around initial hits, optimization process focused on improvement physicochemical properties, cytotoxicity, metabolic stability series. The best compounds obtained exhibited MIC values in low micromolar range, excellent intracellular antimycobacterial activity, an improved profile without cytotoxic effects. Further...
Tuberculosis is the leading cause of death worldwide from infectious diseases. With development drug-resistant strains Mycobacterium tuberculosis, there an acute need for new medicines with novel modes action. Herein, we report discovery and profiling a hydantoin-based family antimycobacterial inhibitors decaprenylphospho-β-d-ribofuranose 2-oxidase (DprE1). In this study, have prepared library more than 100 compounds evaluated them their biological physicochemical properties. The series...
In search of novel drugs against tuberculosis, we previously discovered and profiled a hydantoin-based family that demonstrated highly promising in vitro potency Mycobacterium. tuberculosis. The compounds were found to be noncovalent inhibitors DprE1, subunit decaprenylphosphoryl-β-d-ribose-2′-epimerase. This protein, localized the periplasmic space mycobacterial cell wall, was shown an essential vulnerable antimycobacterial drug target. Here, report further SAR exploration this chemical...
New CCl 3 ‐ and CF ‐substituted enones, bearing additional hidden hydroxymethyl functions, were prepared by acylation of 4‐methylene 1,3‐dioxolanes. The synthesized enones are interesting building blocks for agrochemical medicinal chemistry research. reactivity with various amines was studied, enaminones 13 14 obtained under NH interaction; the reaction aliphatic primary afforded 17 in high yields as equilibrium mixtures E Z isomers. fluorinated enone 9c anilines a mixture products,...
An optimized protocol for the preparation of fluorine‐containing acyclic enones, which are promising building blocks a large variety fluorinated compounds was developed. These enones easily react with secondary amines to form 3‐aminocyclopent‐2‐enones via 4‐amino‐2,3‐dihydrofuran‐2‐ols. The peculiar mechanism involving an intramolecular electrocyclization as key step is proposed.
first_page settings Order Article Reprints Font Type: Arial Georgia Verdana Size: Aa Line Spacing: Column Width: Background: Open AccessExtended Abstract Epigenetic and PPI Targeted Libraries from Life Chemicals † by Vasily Pinchuk *, George Bondar Olga Balabon In., 1a DIXIE AVE, Niagara-on-the-Lake, ON L0S 1J0, Canada * Author to whom correspondence should be addressed. Presented at the 2nd Molecules Medicinal Chemistry Symposium (MMCS): Facing Novel Challenges in Drug Discovery,...