Forrest A K, Jarvest R L, Mensah L M, O'Hanlon P J, Pope A J, Sheppard R J
SmithKline Beecham Pharmaceuticals, Discovery Research, Harlow, Essex, UK.
Bioorg Med Chem Lett. 2000 Aug 21;10(16):1871-4. doi: 10.1016/s0960-894x(00)00360-7.
Aminoalkyl adenylates and aminoacyl sulfamates derived from arginine, histidine and threonine, have been prepared and tested as inhibitors of their cognate Staphylococcus aureus aminoacyl tRNA synthetases. The arginyl derivatives were both potent nanomolar inhibitors of the Class I arginyl tRNA synthetase whereas for the Class II histidyl and threonyl tRNA synthetases, the acyl sulfamates were potent inhibitors but the adenylates had very little affinity.
已制备了源自精氨酸、组氨酸和苏氨酸的氨基烷基腺苷酸和氨基酰基氨基磺酸酯,并将其作为其同源金黄色葡萄球菌氨基酰基tRNA合成酶的抑制剂进行了测试。精氨酰衍生物都是I类精氨酰tRNA合成酶的强效纳摩尔抑制剂,而对于II类组氨酰和苏氨酰tRNA合成酶,氨基酰基氨基磺酸酯是强效抑制剂,但腺苷酸的亲和力很小。