Jarvest R L, Berge J M, Brown P, Hamprecht D W, McNair D J, Mensah L, O'Hanlon P J, Pope A J
GlaxoSmithKline, New Frontiers Science Park, Harlow, Essex, UK.
Bioorg Med Chem Lett. 2001 Mar 12;11(5):715-8. doi: 10.1016/s0960-894x(01)00040-3.
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.
已合成SB - 219383的新型吡喃糖基类似物，以阐明吡喃环周围的构效关系。已鉴定出对细菌酪氨酰tRNA合成酶具有高效立体选择性和抑菌选择性抑制作用的类似物。分子整体极性的大幅降低在不损失纳摩尔级抑制水平的情况下是可以耐受的。
