AI Article Synopsis
- The study focused on modifying pseudomonic acid analogues, replacing specific chemical groups to create new compounds.
- Significant testing was done on these compounds to measure their effectiveness at inhibiting the enzyme isoleucyl tRNA synthetase from Staphylococcus aureus and establishing minimum inhibitory concentrations (MIC).
- Some compounds displayed very low IC50 values, indicating strong inhibition, but had higher MIC values, suggesting they struggled to penetrate bacterial cells effectively.
Article Abstract
The electronic requirements around the C1-C3 region of pseudomonic acid analogues were investigated. Synthetic routes were developed to access a range of compounds where the alpha, beta-unsaturated ester moiety had been replaced by a 5-membered ring heterocycle. The inhibition of isoleucyl tRNA synthetase from Staphylococcus aureus NCTC 6571 was determined as was the minimum inhibitory concentration (MIC) of the test compounds against that organism. Compounds possessing a region of electrostatic potential corresponding to that of the carbonyl group in the alpha, beta-unsaturated ester, and a low-energy unoccupied molecular orbital in the region corresponding to the double bond, were found to have IC50 values of 0.7-5.3 ng mL-1. However the MIC values of these compounds were in the range 2.0-8.0 micrograms mL-1, reflecting their poorer penetration into the bacterial cell.
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| http://dx.doi.org/10.1021/jm960738k | DOI Listing |
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