Novel N-substituted aminopyridine derivatives: synthesis and antibacterial activity
| Author | Affiliation |
|---|---|
Juraitytė, Gabrielė | |
| Date | Volume | Start Page | End Page |
|---|---|---|---|
2023 | 17 | 52 | 52 |
It is well known that new resistant bacterial species are constantly evolving, which poses a threat to the effectiveness of antibiotics [1]. Computational methods are increasingly used to model and predict potential drug candidates. Unfortunately, there is a lack of accuracy in predicting precise structures of active compounds. New molecules can be and still are being created by trying to combine several fragments that have previously shown similar activity. The prepared set of compounds is then tested, and further modifications are planned according to the preliminary results of the biotesting. One of the directions in the development of substances with antibacterial effects is the synthesis of N-heteroaryl-2-arylacetamides [2]. The pyridine fragment is also found in substances possessing antibacterial effects [3]. Preliminary antibacterial properties studies of novel N-heteroaryl-2-arylacetamides have been carried out in collaboration between chemists and microbiologists. In this study, 2-(3-chlorophenyl)-N-(pyridin-2-yl)acetamide and 2-(3-chlorophenyl)-N-(pyridin-4-yl)acetamide were observed to exhibit antibacterial activity against E. coli dh5ɑ bacterial line. Therefore, a new goal was set: to expand the library of investigated N-heteroaryl-2-arylacetamides by adding new analog derivatives aiming to identify correlation of antibacterial properties to the position of the chlorine atom in the benzene ring, the position of the pyridine connection and additional substituents in pyridine ring. To reliably prove the structure of the obtained novel compounds, spectral analysis (NMR, IR) and mass spectrometric analysis (MS) methods were used. All compounds prepared for biological studies were purified to at least 97% purity (LC-MS) and the results of their antibacterial activity against E.coli dh5ɑ bacteria line were evaluated. During the presentation, the synthesis of compounds and the results of biological tests will be discussed.