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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Conformational restriction of methionyl tRNA synthetase inhibitors leading to analogues with potent inhibition and excellent gram-Positive antibacterial activity.
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Conformational restriction of methionyl tRNA synthetase inhibitors leading to analogues with potent inhibition and excellent gram-Positive antibacterial activity.

机译:甲硫氨酰tRNA合成酶抑制剂的构象限制导致类似物具有强力抑制作用和出色的革兰氏阳性抗菌活性。

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摘要

Conformationally restricted analogues of the central linker unit of bacterial methionyl tRNA synthetase (MRS) inhibitors have been prepared. The (1S,2R)-cyclopentylmethyl moiety was identified as the preferred cyclic linker, with significant diastereo- and enantioselectivity of activity. Combination of this linker with an optimal substituted aryl right-hand side has resulted in a compound with exceptionally good antibacterial activity against staphylococci and enterococci, including antibiotic resistant strains.
机译:已经制备了细菌甲硫氨酰tRNA合成酶(MRS)抑制剂的中央接头单元的构象受限的类似物。 (1S,2R)-环戊基甲基部分被确定为优选的环状连接基,具有明显的非对映选择性和对映选择性。该接头与最佳取代的芳基右手侧的组合产生了一种对葡萄球菌和肠球菌具有极佳抗菌活性的化合物,包括抗药性菌株。

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