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Your search keyword '"Elder, John S."' showing total 2 results
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2 results on '"Elder, John S."'

1. Definition of the heterocyclic pharmacophore of bacterial methionyl tRNA synthetase inhibitors: potent antibacterially active non-quinolone analogues

Author

Jarvest, Richard L., Armstrong, Sula A., Berge, John M., Brown, Pamela, Elder, John S., Brown, Murray J., Copley, Royston C.B., Forrest, Andrew K., Hamprecht, Dieter W., O'Hanlon, Peter J., Mitchell, Darren J., Rittenhouse, Stephen, and Witty, David R.

Subjects
*TRANSFER RNA, *QUINOLONE antibacterial agents, *SYNTHETIC drugs, *ENTEROCOCCUS
Abstract

Potent inhibitors of bacterial methionyl tRNA synthetase (MRS) have previously been reported. Through SAR of the quinolone moiety, the right hand side pharmacophore for MRS inhibition has now been defined as an NH–C–NH functionality in the context of a bicyclic heteroaromatic system. Potent antibacterial fused-pyrimidone and fused-imidazole analogues have been obtained and enantioselective activity demonstrated. Compound 46 demonstrated very good antibacterial activity against panels of antibiotic-resistant staphylococci and enterococci. [Copyright &y& Elsevier]

Published
2004
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2. Optimisation of aryl substitution leading to potent methionyl tRNA synthetase inhibitors with excellent gram-Positive antibacterial activity

Author

Jarvest, Richard L., Berge, John M., Brown, Murray J., Brown, Pamela, Elder, John S., Forrest, Andrew K., Houge-Frydrych, C.S.V., O'Hanlon, Peter J., McNair, David J., Rittenhouse, Stephen, and Sheppard, Robert J.

Subjects
*ARYLATION, *STAPHYLOCOCCUS aureus
Abstract

Optimisation of the left-hand-side aryl moiety of a file compound screening hit against Staphylococcus aureus methionyl tRNA synthetase led to the identification of a series of potent nanomolar inhibitors. The best compounds showed excellent antibacterial activity against staphylococcal and enterococcal pathogens, including strains resistant to clinical antibiotics. [Copyright &y& Elsevier]

Published
2003
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