Design, Synthesis and Microbiological Evaluation of Novel Compounds as Potential Staphylococcus aureus Phenylalanine tRNA Synthetase Inhibitors
AS THE RESISTANCE of 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 PheRS to aid the design proce...
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| Veröffentlicht in: | Egyptian Journal of Chemistry 2018-11, Vol.61 (Conference Iss), p.9-25 |
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| container_title | Egyptian Journal of Chemistry |
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| creator | Elbaramawi, Samar S Hughes, Casey Richards, Jennifer Gupta, Arya Ibrahim, Samy M Lashine, El-Sayed M El-Sadek, Mohamed E O'Neill, Alex J Wootton, Mandy Bullard, James M Simons, Claire |
| description | AS THE RESISTANCE of
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
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
H NMR,
C NMR, HRMS and/or microanalysis, and they were microbiologically evaluated. |
| doi_str_mv | 10.21608/EJCHEM.2018.4070.1357 |
| format | Article |
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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
H NMR,
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| source | Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals |
| title | Design, Synthesis and Microbiological Evaluation of Novel Compounds as Potential Staphylococcus aureus Phenylalanine tRNA Synthetase Inhibitors |
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