Synthesis and activity of analogues of SB-219383: Novel potent inhibitors of bacterial tyrosyl tRNA synthetase

被引:22
作者
Berge, JM [1 ]
Broom, NJP [1 ]
Houge-Frydrych, CSV [1 ]
Jarvest, RL [1 ]
Mensah, L [1 ]
McNair, DJ [1 ]
O'Hanlon, PJ [1 ]
Pope, AJ [1 ]
Rittenhouse, S [1 ]
机构
[1] SmithKline Beecham Pharmaceut, Harlow CM19 5AW, Essex, England
关键词
D O I
10.7164/antibiotics.53.1282
中图分类号
Q81 [生物工程学(生物技术)]; Q93 [微生物学];
学科分类号
071005 ; 0836 ; 090102 ; 100705 ;
摘要
SB-219383 is a naturally occurring antibiotic, which acts by inhibition of tyrosyl tRNA synthetase. Semi-synthetic derivatives of SB-219383 were prepared with the objective of elucidating the key features required for inhibition of tyrosyl tRNA synthetase in order to improve the antibacterial activity. Some ester and amide derivatives as well as monocyclic analogues exhibited sub-nanomolar inhibitory activity against tyrosyl tRNA synthetase.
引用
收藏
页码:1282 / 1292
页数:11
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