Aminoalkyl adenylate and aminoacyl sulfamate intermediate analogues differing greatly in affinity for their cognate Staphylococcus aureus aminoacyl tRNA synthetases

被引:58
作者
Forrest, AK [1 ]
Jarvest, RL [1 ]
Mensah, LM [1 ]
O'Hanlon, PJ [1 ]
Pope, AJ [1 ]
Sheppard, RJ [1 ]
机构
[1] SmithKline Beecham Pharmaceut, Harlow CM19 5AW, Essex, England
关键词
D O I
10.1016/S0960-894X(00)00360-7
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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. (C) 2000 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1871 / 1874
页数:4
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