Design, Synthesis and Microbiological Evaluation of Novel Compounds as Potential Staphylococcus aureus Phenylalanine tRNA Synthetase Inhibitors

Authors

• Samar S. Elbaramawi, College of Biomedical and Life Sciences
• Casey Hughes, The University of Texas Rio Grande Valley
• Jennifer Richards, University Hospital of Wales
• Arya Gupta, University of Leeds
• Samy M. Ibrahim, Faculty of Pharmacy
• El Sayed M. Lashine, Faculty of Pharmacy
• Mohamed E. El-Sadek, Faculty of Pharmacy
• Alex J. O’Neill, University of Leeds
• Mandy Wootton, University Hospital of Wales
• James M. Bullard, The University of Texas Rio Grande ValleyFollow

Document Type

Article

Publication Date

12-1-2018

Abstract

AS THE RESISTANCE of Staphylococcus aureus to antibiotics represents a major threat to global health, anti-infectives with novel mechanisms must be developed. Novel compounds were generated as potential phenylalanine tRNA synthetase (PheRS) inhibitors based on the published homology model of S. aureus PheRS to aid the design process using Molecular Operating Environment (MOE) software. PheRS was selected as it is structurally unique enzyme among the aminoacyl-tRNA synthetases (aaRS), it is considerably different from human cytosolic and human mitochondrial aaRS and it is essential and conserved across bacterial species. The designed compounds were synthesized according to different clear schemes. The compounds were confirmed by ¹H NMR, ¹³C NMR, HRMS and/or microanalysis, and they were microbiologically evaluated.

Recommended Citation

Elbaramawi, Samar S., Casey Hughes, Jennifer Richards, et al. “Design, Synthesis and Microbiological Evaluation of Novel Compounds as Potential Staphylococcus Aureus Phenylalanine tRNA Synthetase Inhibitors.” Egyptian Journal of Chemistry 61, no. Conference Iss (2018): 9–25. https://doi.org/10.21608/EJCHEM.2018.4070.1357.

First Page

9

Last Page

25

Publication Title

Egyptian Journal of Chemistry

DOI

10.21608/EJCHEM.2018.4070.1357