Potent synthetic inhibitors of tyrosyl tRNA synthetase derived from C-pyranosyl analogues of SB-219383 |
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| Authors: | Jarvest R L Berge J M Brown P Hamprecht D W McNair D J Mensah L O'Hanlon P J Pope A J |
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| Affiliation: | GlaxoSmithKline, New Frontiers Science Park, Harlow, Essex, UK. pam_brown-1@sbphrd.com |
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| Abstract: | Novel pyranosyl analogues of SB-219383 have been synthesised to elucidate the structure-activity relationships around the pyran ring. Analogues with highly potent stereoselective and bacterioselective inhibition of bacterial tyrosyl tRNA synthetase have been identified. A major reduction in the overall polarity of the molecule can be tolerated without loss of the nanomolar level of inhibition. |
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