Abstract
In this study, a series of 3-(3-pyridyl)-oxazolidone-5-methyl ester derivatives was synthesized and characterized by 1H NMR, 13C NMR, and LC-MS. The conducted screening antibacterial studies of the new 3-(3-pyridyl)-oxazolidone-5-methyl ester derivatives established that the methyl sulfonic acid esters have broad activity spectrum towards Staphylococcus aureus, Streptococcus pneumoniae, Bacillus subtilis and Staphylococcus epidermidis. Among them, compound 12e has the most potent activity, with an MIC of 16 μg/mL against B.subtilis, and could reduce the instantaneous growth rate of bacteria. Furthermore, molecular docking studies were also simulated for compound 12e to predict the specific binding mode of this compound. In addition, anthelmintic activity of these compounds was also evaluated against adult Indian earthworms (Pheretima posthuman). The results showed that compound 11b had the best effect. These results above can provide experimental reference for the development of novel antibacterial and anthelmintic drugs.
Highlights
With bacterial resistance comes a grave threat to global public health security
Seventeen novel 3-(3-pyridyl)-oxazolidone-5-methyl derivatives were designed and synthesized, and their structures were identified by 1H NMR, 13C NMR and mass spectra (MS)
The primary screening of antibacterial activity, which was tested on Staphylococcus aureus (ATCC25923), Streptococcus pneumoniae (ATCC49619), Bacillus subtilis (BNCC109047) and Staphylococcus epidermidis (BNCC186652), showed that most of the compounds had certain antibacterial activity, among which compound 12a and 12e had the best antimicrobial activity
Summary
With bacterial resistance comes a grave threat to global public health security. Owing to the rapid growth of clinical drug-resistant bacteria, the number of effective anti-infective drugs has declined, and patient mortality is increasing [1,2,3,4,5]. How to effectively deal with the bacterial resistance crisis is a challenging question. Many new therapies, such as those utilizing nanoparticles, phages, and protic ionic liquids, are being developed [7,8,9,10,11]. These technologies are still immature and have not been effectively used clinically [12,13,14]. For pharmaceutical chemists all over the world, the discovery of novel active antibacterial compounds is an urgent mission and the direction of continuous efforts
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